nms

NMS publications

2017

  • Phase I dose escalation study of NMS-1286937

    Phase I dose escalation study of NMS-1286937, an orally available Polo-Like Kinase 1 inhibitor, in patients with advanced or metastatic solid tumors
    Weiss GJ, Jameson G, Von Hoff DD, Valsasina B, Davite C, Di Giulio C, Fiorentini F, Alzani R, Carpinelli P, Di Sanzo A, Galvani A, Isacchi A, Ramanathan RK
    CInvest New Drugs (2017) Epub ahead of print
    View abstract on PubMed

    Establishment and genomic characterization of the new chordoma cell line

    Establishment and genomic characterization of the new chordoma cell line Chor-IN-1
    Bosotti R, Magnaghi P, Di Bella S, Cozzi L, Cusi C, Bozzi F, Beltrami N, Carapezza G, Ballinari D, Amboldi N, Lupi R, Somaschini A, Raddrizzani L, Salom B, Galvani A, Stacchiotti S, Tamborini E, Isacchi A
    Sci Rep (2017), 7(1), 9226
    View abstract on PubMed

    Multivalency Increases the Binding Strength

    Multivalency Increases the Binding Strength of RGD Peptidomimetic-Paclitaxel Conjugates to Integrin αV β3
    Raposo Moreira Dias A, Pina A, Dal Corso A, Arosio D, Belvisi L, Pignataro L, Caruso M, Gennari C.
    Chemistry, (2017), 23(58), 14410-14415
    View abstract on PubMed

    Identification and characterization of a novel SCYL3-NTRK1 rearrangement

    Identification and characterization of a novel SCYL3-NTRK1 rearrangement in a colorectal cancer patient
    Milione M, Ardini E, Christiansen J, Valtorta E, Veronese S, Bosotti R, Pellegrinelli A, Testi A, Pietrantonio F, Fucà G, Wei G, Murphy D, Siena S, Isacchi A, De Braud F
    Oncotarget (2017), 8(33), 55353-55360
    View abstract on PubMed

    A covalent PIN1 inhibitor selectively targets cancer cells

    A covalent PIN1 inhibitor selectively targets cancer cells by a dual mechanism of action
    Campaner E, Rustighi A, Zannini A, Cristiani A, Piazza S, Ciani Y, Kalid O, Golan G, Baloglu E, Shacham S, Valsasina B, Cucchi U, Pippione AC, Lolli ML, Giabbai B, Storici P, Carloni P, Rossetti G, Benvenuti F, Bello E, D'Incalci M, Cappuzzello E, Rosato A, Del Sal G
    Nat Commun (2017), 8, 15772
    View abstract on PubMed

    FOXM1 expression is significantly associated with chemotherapy resistance

    FOXM1 expression is significantly associated with chemotherapy resistance and adverse prognosis in non-serous epithelial ovarian cancer patients
    Tassi RA, Todeschini P, Siegel ER, Calza S, Cappella P, Ardighieri L, Cadei M, Bugatti M, Romani C, Bandiera E, Zanotti L, Tassone L, Guarino D, Santonocito C, Capoluongo ED, Beltrame L, Erba E, Marchini S, D'Incalci M, Donzelli C, Santin AD, Pecorelli S, Sartori E, Bignotti E, Odicino F, Ravaggi A
    J Exp Clin Cancer Res (2017), 36(1), 63
    View abstract on PubMed

    Tumor Targeting with an isoDGR-Drug Conjugate

    Tumor Targeting with an isoDGR-Drug Conjugate
    Zanella S, Angerani S, Arianna P, López Rivas P, Giannini C, Panzeri S, Arosio D, Caruso M, Gasparri F, Fraietta I, Albanese C, Marsiglio A, Pignataro L, Belvisi L, Piarulli U, Gennari C.
    Chemistry (2017), 23, 7910-7914
    View abstract on PubMed

    Combined cisplatin and aurora inhibitor treatment increase neuroblastoma cell

    The novel PIM1 inhibitor NMS-P645 reverses PIM1-dependent effects on TMPRSS2/ERG positive prostate cancer cells and shows anti-proliferative activity in combination with PI3K inhibition
    Mologni L, Magistroni V, Casuscelli F, Montemartini M, Gambacorti-Passerini C
    J Cancer (2017), 8(1), 140-145
    View abstract on PubMed

    Combined cisplatin and aurora inhibitor treatment increase neuroblastoma cell

    Virtual cross-linking of the active Nemorubicin metabolite PNU-159682 to double-stranded DNAs
    Scalabrin M, Quintieri L, Palumbo M, Riccardi Sirtori F, Gatto B
    Chem. Res. Toxico (2017), 30 (2), 614–624
    View abstract on PubMed

    Combined cisplatin and aurora inhibitor treatment increase neuroblastoma cell

    Safety and antitumor activity of the multi-targeted Pan-TRK, ROS1, and ALK inhibitor Entrectinib (RXDX-101): combined results from two phase 1 trials (ALKA-372-001 and STARTRK-1)
    Drilon A, Siena S, Ou SI, Patel M, Ahn MJ, Lee J, Bauer TM, Farago AF, Wheler JJ, Liu SV, Doebele R, Giannetta L, Cerea G, Marrapese G, Schirru M, Amatu A, Bencardino K, Palmeri L, Sartore-Bianchi A, Vanzulli A, Cresta S, Damian S, Duca M, Ardini E, Li G, Christiansen J, Kowalski K, Johnson A, Patel R1, Luo D, Chow-Maneval E, Hornby Z, Multani PS, Shaw AT, De Braud FG
    Cancer Discov (2017), (7)4, 400-409
    View abstract on PubMed

    Combined cisplatin and aurora inhibitor treatment increase neuroblastoma cell

    miR-494-3p is a novel tumor driver of lung carcinogenesis
    Faversani A, Amatori S, Augello C, Colombo F, Porretti L, Fanelli M, Ferrero S, Palleschi A, Pelicci PG, Belloni E, Ercoli G, Degrassi A, Baccarin M, Altieri DC, Vaira V, Bosari S
    Oncotarget. (2017), 8(5), 7231-7247
    View abstract on PubMed

Archive 2016

Combined cisplatin and aurora inhibitor treatment increase neuroblastoma cell

KAOS: a new automated computational method for the identification of overexpressed genes
Nuzzo A, Carapezza G, Di Bella S, Pulvirenti A3, Isacchi A, Bosotti R
BMC Bioinformatics (2016), 17(Suppl 12), 340
View abstract on PubMed

Combined cisplatin and aurora inhibitor treatment increase neuroblastoma cell

Sensitivity to Entrectinib associated with a novel LMNA-NTRK1 gene fusion in metastatic colorectal cancer
Sartore-Bianchi A, Ardini E, Bosotti R, Amatu A, Valtorta E, Somaschini A, Raddrizzani L, Palmeri L, Banfi P, Bonazzina E, Misale S, Marrapese G, Leone A, Alzani R, Luo D, Hornby Z, Lim J, Veronese S, Vanzulli A, Bardelli A, Martignoni M, Davite C, Galvani A, Isacchi A, Siena S
J Natl Cancer Inst (2016), 108(1), 1-4
View abstract on PubMed

Combined cisplatin and aurora inhibitor treatment increase neuroblastoma cell

Combined cisplatin and aurora inhibitor treatment increase neuroblastoma cell death but surviving cells overproduce BDNF
Polacchini A, Albani C, Baj G, Colliva A, Carpinelli P, Tongiorgi E.,
Biol Open. (2016), 5(7), 899-90
View abstract on PubMed

Current Deep Sequencing Data Analysis

Noncoding RNA: Current Deep Sequencing Data Analysis Approaches and Challenges
Veneziano D, Di Bella S, Nigita G, Laganà A, Ferro A, Croce CM.
Hum Mutat (2016), 37(12),1283-1298
View abstract on PubMed

Nemorubicin and doxorubicin bind the G-quadruplex sequences of the human telomeres

Nemorubicin and doxorubicin bind the G-quadruplex sequences of the human telomeres and of the c-MYC promoter element Pu22
Scaglioni L, Mondelli R, Artali R, Sirtori FR, Mazzini S
Biochim Biophys Acta. (2016), 1860(6), 1129-38
View abstract on PubMed

identification and quantification of 2-hydroxyglutarate in L-2-Hydroxyglutaric aciduria

In-vivo brain H1-MR-Spectroscopy identification and quantification of 2-hydroxyglutarate in L-2-Hydroxyglutaric aciduria
Anghileri E, Bertolino N, Salsano E, Antelmi L, Carpinelli P, Castellotti B, Zucca I, Gellera C, Bisogno R, Caccia C, Cuccarini V
Brain Res (2016), 1648(Pt A), 506-11
View abstract on PubMed

Computational drugs  identifies inhibitors of PI3K/AKT/P70S6K-dependent pathways

Computational drugs repositioning identifies inhibitors of oncogenic PI3K/AKT/P70S6K-dependent pathways among FDA-approved compounds
Carrella D, Manni I, Tumaini B, Dattilo R, Papaccio F, Mutarelli M, Sirci F, Amoreo CA, Mottolese M, Iezzi M, Ciolli L, Aria V, Bosotti R, Isacchi A, Loreni F, Bardelli A, Avvedimento VE, di Bernardo D, Cardone L
Oncotarget (2016), 7(37), 58743-58758
View abstract on PubMed

MutT Homolog 1 (MTH1): The Silencing of a Target

MutT Homolog 1 (MTH1): The Silencing of a Target
Papeo G
J Med Chem (2016), 59, 2343.2345
View abstract on PubMed

Immunological Characterization of Whole Tumour Lysate-Loaded Dendritic Cells for Cancer Immunotherap

Immunological Characterization of Whole Tumour Lysate-Loaded Dendritic Cells for Cancer Immunotherapy
Rainone V, Martelli C, Ottobrini L, Biasin M, Borelli M, Lucignani G, Trabattoni D, Clerici M
PLoS One (2016), 11(1), e0146622. Erratum in: PLoS One. (2016) 11(3), e0151008
View abstract on PubMed

 Immunological Characterization of Whole Tumour Lysate-Loaded Dendritic Cells for Cancer Immunotherapy

Correction: Immunological Characterization of Whole Tumour Lysate-Loaded Dendritic Cells for Cancer Immunotherapy
Rainone V, Martelli C, Ottobrini L, Biasin M, Texido G, Degrassi A, Borelli M, Lucignani G, Trabattoni D, Clerici M
PLoS One (2015), 10(10), 1-14
View abstract on PubMed

Discovery of Entrectinib: A New 3-Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK)

Discovery of Entrectinib: A New 3-Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor
Menichincheri M, Ardini E, Magnaghi P, Avanzi N, Banfi P, Bossi R, Buffa L, Canevari G, Ceriani L, Colombo M, Corti L, Donati D, Fasolini M, Felder E, Fiorelli C, Fiorentini F, Galvani A, Isacchi A, Borgia AL, Marchionni C, Nesi M, Orrenius C, Panzeri A, Pesenti E, Rusconi L, Saccardo MB, Vanotti E, Perrone E, Orsini P
J Med Chem (2016), 59(7), 3392-408
View abstract on PubMed

Entrectinib, a Pan-TRK, ROS1, and ALK Inhibitor

Entrectinib, a Pan-TRK, ROS1, and ALK Inhibitor with Activity in Multiple Molecularly Defined Cancer Indications
Ardini E, Menichincheri M, Banfi P, Bosotti R, De Ponti C, Pulci R, Ballinari D, Ciomei M, Texido G, Degrassi A, Avanzi N, Amboldi N, Saccardo MB, Casero D, Orsini P, Bandiera T, Mologni L, Anderson D, Wei G, Harris J, Vernier JM, Li G, Felder E, Donati D, Isacchi A, Pesenti E, Magnaghi P, Galvani A
J Mol Cancer Ther. (2016),15(4), 628-39
View abstract on PubMed

The development of high-content screening (HCS) technology

The development of high-content screening (HCS) technology and its importance to drug discovery
Fraietta I, Gasparri F
Expert Opin Drug Discov (2016), 11(5), 501-14
View abstract on PubMed

Archive 2015

Novel CAD-ALK gene rearrangement is drugable by entrectinib in colorectal cancer

Editorial: BITS2014, the annual meeting of the Italian Society of Bioinformatics
Facchiano A, Angelini C, Bosotti R, Guffanti A, Marabotti A, Marangoni R, Pascarella S, Romano P, Zanzoni A, Helmer-Citterich M
Bioinformatics (2015), 16(Suppl) 9), S1
View abstract on PubMed

Novel CAD-ALK gene rearrangement is drugable by entrectinib in colorectal cancer

Novel CAD-ALK gene rearrangement is drugable by entrectinib in colorectal cancer
Amatu A, Somaschini A, Cerea G, Bosotti R, Valtorta E, Buonandi P, Marrapese G, Veronese S, Luo D, Hornby Z, Multani P, Murphy D, Shoemaker R, Lauricella C, Giannetta L, Maiolani M, Vanzulli A, Ardini E, Galvani A, Isacchi A, Sartore-Bianchi A, Siena S
Br J Cancer. (2015), 113(12), 1730-4
View abstract on PubMed

A Novel High-Content Immunofluorescence A
ssay

A Novel High-Content Immunofluorescence Assay as a Tool to Identify at the Single Cell Level γ-Globin Inducing Compounds
Durlak M, Fugazza C, Elangovan S, Marini MG, Marongiu MF, Moi P, Fraietta I, Cappella P, Barbarani G, Font-Monclus I, Mauri M, Ottolenghi S, Gasparri F, Ronchi A.
PLoS One (2015), 10(10), 1-14
View abstract on PubMed

Identification of thyroid tumor cell vulnerabilities

Identification of thyroid tumor cell vulnerabilities through a siRNA-based functional screening
Anania M, Gasparri F, Cetti E, Fraietta I, Todoerti K, Miranda C, Mazzoni M, Re C, Colombo R, Ukmar G, Camisasca S, Pagliardini S, Pierotti M, Neri A, Galvani A, Greco A.
Oncotarget (2015), 6(33), 34629-34648
View abstract on PubMed

Discovery of NMS-P118

Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP-1 Inhibitor for Cancer Therapy
Papeo G, Posteri H, Borghi D, Busel AA, Caprera F, Casale E, Ciomei M, Cirla A, Corti E, D'Anello M, Fasolini M, Forte B, Galvani A, Isacchi A, Khvat A, Krasavin MY, Lupi R, Orsini P, Perego R, Pesenti E, Pezzetta D, Rainoldi S, Riccardi-Sirtori F, Scolaro A, Sola F, Zuccotto F, Felder ER, Donati D, Montagnoli A
J Med Chem (2015), 58(17), 6875-98
View abstract on PubMed

Establish an automated flow injection ESI-MS method

Establish an automated flow injection ESI-MS method for the screening of fragment based libraries: Application to Hsp90
Riccardi Sirtori F, Caronni D, Colombo M, Dalvit C, Paolucci M, Regazzoni L, Visco C, Fogliatto G
Eur J Pharm Sci (2015), 30(76), 83-94
View abstract on PubMed

A phase I study of danusertib (PHA-739358) in adult patients

A phase I study of danusertib (PHA-739358) in adult patients with accelerated or blastic phase chronic myeloid leukemia and Philadelphia chromosome-positive acute lymphoblastic leukemia resistant or intolerant to imatinib and/or other second generation c-ABL therapy
Borthakur G, Dombret H, Schafhausen P, Brummendorf TH, Boissel N, Jabbour E, Mariani M, Capolongo L, Carpinelli P, Davite C, Kantarjian H, Cortes JE
Haematologica (2015), 100(7), 898-904
View abstract on PubMed

Novel pyrrole carboxamide inhibitors of JAK2

Novel pyrrole carboxamide inhibitors of JAK2 as potential treatment of myeloproliferative disorders
Brasca MG, Gnocchi P, Nesi M, Amboldi N, Avanzi N, Bertrand J, Bindi S, Canevari G, Casero D, Ciomei M, Colombo N, Cribioli S, Fachin G, Felder ER, Galvani A, Isacchi A, Motto I, Panzeri A, Donati D.
Bioorg Med Chem (2015), 15;23(10), 2387-407
View abstract on PubMed

A Novel Anti-CD22 Anthracycline-Based Antibody-Drug Conjugate

A Novel Anti-CD22 Anthracycline-Based Antibody-Drug Conjugate (ADC) That Overcomes Resistance to Auristatin-Based ADCs
Yu SF, Zheng B, Go M, Lau J, Spencer S, Raab H, Soriano R, Jhunjhunwala S, Cohen R, Caruso M, Polakis P, Flygare J, Polson AG
Clin Cancer Res (2015), 21(14), 3298-306
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Synthesis and biological evaluation of RGD peptidomimetic-paclitaxel conjugates

Synthesis and biological evaluation of RGD peptidomimetic-paclitaxel conjugates bearing lysosomally cleavable linkers
Dal Corso A, Caruso M, Belvisi L, Arosio D, Piarulli U, Albanese C, Gasparri F, Marsiglio A, Sola F, Troiani S, Valsasina B, Pignataro L, Donati D, Gennari C.
Chemistry (2015), 21(18), 6921-9
View abstract on PubMed

modulating DNA repair proteins

Targeting MPS1 enhances radiosensitization of human glioblastoma by modulating DNA repair proteins
Maachani UB, Kramp T, Hanson R, Zhao S, Celiku O, Shankavaram U, Colombo R, Caplen NJ, Camphausen K, Tandle A
Mol Cancer Res. 2015 May;13(5):852-62. doi: 10.1158/1541-7786.MCR-14-0462-T. Epub 2015 Feb 26
View abstract on PubMed

IDH1 mutation R132H in a murine model of intracranial glioma

Effective immuno-targeting of the IDH1 mutation R132H in a murine model of intracranial glioma
Pellegatta S1, Valletta L, Corbetta C, Patanè M, Zucca I, Riccardi Sirtori F, Bruzzone MG, Fogliatto G, Isacchi A, Pollo B, Finocchiaro G.
Acta Neuropathol Commun (2015), 3(1),180
View abstract on PubMed

Vascular Endothelial Growth Factor C Promotes Ovarian Carcinoma Progression

Mcl-1 antagonism Is a potential therapeutic strategy in a subset of solid cancers
Modugno M, Banfi P, Gasparri F, Borzilleri R, Carter P, Cornelius L, Gottardis M, Lee V, Mapelli C, Naglich JG, Tebben A, Vite G, Pastori W, Albanese C, Corti E, Ballinari D, Galvani A
Exp Cell Res (2015), 332(2), 267-77
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Vascular Endothelial Growth Factor C Promotes Ovarian Carcinoma Progression

Optimization of Diarylthiazole B-Raf Inhibitors: Identification of a Compound Endowed with High Oral Antitumor Activity, Mitigated hERG Inhibition, and Low Paradoxical Effect
Pulici M, Traquandi G, Marchionni C, Modugno M, Lupi R, Amboldi N, Casale E, Colombo N, Corti L, Fasolini M, Gasparri F, Pastori W, Scolaro A, Donati D, Felder E, Galvani A, Isacchi A, Pesenti E, Ciomei M.
ChemMedChem (2015), 10(2), 276-95
View abstract on PubMed

Archive 2014

!-
a new class of reversible valosine containing protein inhibitors

Discovery of 2-(cyclohexylmethylamino)pyrimidines as a new class of reversible valosine containing protein inhibitors
Cervi G, Magnaghi P, Asa D, Avanzi N, Badari A, Borghi D, Caruso M, Cirla A, Cozzi L, Felder E, Galvani A, Gasparri F, Lomolino A, Magnuson S, Malgesini B, Motto I, Pasi M, Rizzi S, Salom B, Sorrentino G, Troiani S, Valsasina B, O'Brien T, Isacchi A, Donati D, D'Alessio R
J Med Chem (2014), 57(24),10443-54
View abstract on PubMed

Vascular Endothelial Growth Factor C Promotes Ovarian Carcinoma Progression

Drug resistance
Texidó G, Moll J.
Drug Discov Today Technol (2014), 11, 1-3
View abstract on PubMed

Vascular Endothelial Growth Factor C Promotes Ovarian Carcinoma Progression

Direct involvement of CD56 in CIK-mediated lysis of CD56+ hematopoietic target cells
Valgardsdottir R, Capitanio C, Texido G, Pende D, Cantoni C, Pesenti E, Rambaldi A, Golay J, Introna M.
Exp Hematol. (2014), [Epub ahead of print]
View abstract on PubMed

A novel method using blinatumomab for efficient, clinical-grade expansion of polyclonal T cells for adoptive immunotherapy

A novel method using blinatumomab for efficient, clinical-grade expansion of polyclonal T cells for adoptive immunotherapy
Golay J, D'Amico A, Borleri G, Bonzi M, Valgardsdottir R, Alzani R, Cribioli S, Albanese C, Pesenti E, Finazzi MC, Quaresmini G, Nagorsen D, Introna M, Rambaldi A.
J Immunol. (2014), 193(9), 4739-47
View abstract on PubMed

Vascular Endothelial Growth Factor C Promotes Ovarian Carcinoma Progression

The TPM3-NTRK1 rearrangement is a recurring event in colorectal carcinoma and is associated with tumor sensitivity to TRKA kinase inhibition
Ardini E, Bosotti R, Borgia AL, De Ponti C, Somaschini A, Cammarota R, Amboldi N, Raddrizzani L, Milani A, Magnaghi P, Ballinari D, Casero D, Gasparri F, Banfi P, Avanzi N, Saccardo MB, Alzani R, Bandiera T, Felder E, Donati D, Pesenti E, Sartore-Bianchi A, Gambacorta M, Pierotti MA, Siena S, Veronese S, Galvani A, Isacchi A. .
Mol Oncol. (2014), 8(8), 1495-507
View abstract on PubMed

Vascular Endothelial Growth Factor C Promotes Ovarian Carcinoma Progression

Targeting polo-like kinase 1 by NMS-P937 in osteosarcoma cell lines inhibits tumor cell growth and partially overcomes drug resistance
Sero V, Tavanti E, Vella S, Hattinger CM, Fanelli M, Michelacci F, Versteeg R, Valsasina B, Gudeman B, Picci P, Serra M
Invest New Drugs. (2014) 32(6), 1167-80
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Vascular Endothelial Growth Factor C Promotes Ovarian Carcinoma Progression

Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors
Casale E, Amboldi N, Brasca MG, Caronni D, Colombo N, Dalvit C, Felder ER, Fogliatto G, Galvani A, Isacchi A, Polucci P, Riceputi L, Sola F, Visco C, Zuccotto F, Casuscelli F.
Bioorg Med Chem. (2014), 22(15), 4135-50
View abstract on PubMed

Vascular Endothelial Growth Factor C Promotes Ovarian Carcinoma Progression

Pyrrole-3-carboxamides as potent and selective JAK2 inhibitors
Brasca MG, Nesi M, Avanzi N, Ballinari D, Bandiera T, Bertrand J, Bindi S, Canevari G, Carenzi D, Casero D, Ceriani L, Ciomei M, Cirla A, Colombo M, Cribioli S, Cristiani C, Della Vedova F, Fachin G, Fasolini M, Felder ER, Galvani A, Isacchi A, Mirizzi D, Motto I, Panzeri A, Pesenti E, Vianello P, Gnocchi P, Donati D.
Bioorg Med Chem. (2014), 22(14), 4998-5012
View abstract on PubMed

Vascular Endothelial Growth Factor C Promotes Ovarian Carcinoma Progression

Vascular Endothelial Growth Factor C Promotes Ovarian Carcinoma Progression through Paracrine and Autocrine Mechanisms
Decio A, Taraboletti G, Patton V, Alzani R, Perego P, Fruscio R, Jürgensmeier JM, Giavazzi R, Belotti D.
Am J Pathol. (2014) 184(4), 1050-61
View abstract on PubMed

elective Inhibition of Pancreatic Ductal Adenocarcinoma

Selective Inhibition of Pancreatic Ductal Adenocarcinoma Cell Growth by the Mitotic MPS1 Kinase Inhibitor NMS-P715
Slee RB, Grimes BR, Bansal R, Gore J, Blackburn C, Brown L, Gasaway R, Jeong J, Victorino J, March KL, Colombo R, Herbert BS, Korc M.
Mol Cancer Ther (2014), 13(2), 307-15
View abstract on PubMed

Highly multiplexed phenotypic imaging

Highly multiplexed phenotypic imaging for cell proliferation studies
Cappella P, Gasparri F.
J Biomol Screen (2014), 19(1), 145-57
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New resistance mechanisms for small molecule kinase inhibitors

New resistance mechanisms for small molecule kinase inhibitors of Abl kinase Review Article
Modugno M
Drug Discovery Today: Technologies (2014), 11, 5-10
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Accuracy of 2-hydroxyglutarate quantification

Accuracy of 2-hydroxyglutarate quantification by short-echo proton-MRS at 3 T: A phantom study
Bertolino N, Marchionni C, Ghielmetti F, Burns B, Finocchiaro G, Anghileri E, Bruzzone MG, Minati L.
Phys Med. (2014), 30(6), 702-7
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Insights into PARP Inhibitors' Selectivity

Insights into PARP Inhibitors' Selectivity Using Fluorescence Polarization and Surface Plasmon Resonance Binding Assays
Papeo G, Avanzi N, Bettoni S, Leone A, Paolucci M, Perego R, Quartieri F, Riccardi-Sirtori F, Thieffine S, Montagnoli A, Lupi R.
J Biomol Screen. (2014), 19 (8), 1212-1219
View abstract on PubMed

Archive 2013

9-Fluorenone-2-Carboxylic Acid

9-Fluorenone-2-Carboxylic Acid as a Scaffold for Tubulin Interacting Compounds
Calogero F, Borrelli S, Speciale G, Christodoulou MS, Cartelli D, Ballinari D, Sola F, Albanese C, Ciavolella A, Passarella D, Cappelletti G, Pieraccini S, Sironi M
ChemPlusChem (2013), 78(7), 663–669

Computer-aided design, synthesis and validation of 2-phenylquinazolinone fragments

Computer-aided design, synthesis and validation of 2-phenylquinazolinone fragments as CDK9 inhibitors with anti-HIV-1 Tat-mediated transcription activity
Sancineto L, Iraci N, Massari S, Attanasio V, Corazza G, Barreca ML, Sabatini S, Manfroni G, Avanzi NR, Cecchetti V, Pannecouque C, Marcello A, Tabarrini O.
ChemMedChem (2013), 8(12), 1941-53
View abstract on PubMed

Zebularine partially reverses GST methylation

Zebularine partially reverses GST methylation in prostate cancer cells and restores sensitivity to the DNA minor groove binder brostallicin
Sabatino MA, Geroni C, Ganzinelli M, Ceruti R, Broggini M.
Epigenetics (2013), 8(6), 656-65
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Diffuse scaling dermatitis

Italian chemists' contributions to named reactions in organic synthesis: an historical perspective
Papeo G, Pulici M.
Molecules (2013), 8(9), 10870-900
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Discovery of NMS-E973 as novel

Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90)
Brasca MG, Mantegani S, Amboldi N, Bindi S, Caronni D, Casale E, Ceccarelli W, Colombo N, De Ponti A, Donati D, Ermoli A, Fachin G, Felder ER, Ferguson RD, Fiorelli C, Guanci M, Isacchi A, Pesenti E, Polucci P, Riceputi L, Sola F, Visco C, Zuccotto F, Fogliatto G.
Bioorg Med Chem. (2013), 21(22), 7047-63
View abstract on PubMed

Discovery

Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases
Casuscelli F, Ardini E, Avanzi N, Casale E, Cervi G, D’Anello M, Donati D, Faiardi D, Ferguson RD, Fogliatto GP, Galvani A, Marsiglio A, Mirizzi D, Montemartini M, Orrenius C, Papeo G, Piutti C, Salom B, Felder ER
Bioorganic & Medicinal Chemistry (2013), 21(23), 7364-80
Sciencedirect

The Piancatelli rearrangement

The Piancatelli rearrangement: new applications for an intriguing reaction
Piutti C, Quartieri F
Molecules (2013), 18, 12290-12312

Diffuse scaling dermatitis

Diffuse scaling dermatitis in an athymic nude mouse.
Russo M, Invernizzi A, Gobbi A, Radaelli E.
Vet Pathol. (2013), 50(4), 722-6
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embryonic leucine zipper kinase (MELK)

Structural insight into maternal embryonic leucine zipper kinase (MELK) conformation and inhibition toward structure-based drug design
Canevari G, Re Depaolini S, Cucchi U, Bertrand JA, Casale E, Perrera C, Forte B, Carpinelli P, Felder ER
Biochemistry (2013), 52(37), 6380-7
View abstract on PubMed

Diffuse scaling dermatitis

From "Click" to "Fenton" chemistry for 5-bromo-2'-deoxyuridine determination
Cappella P, Giansanti V, Pulici M, Gasparri F.
Cytometry A (2013), 83(11), 989-1000
View abstract on PubMed

allosteric inhibitors of the ATPase VCP/p97

Covalent and allosteric inhibitors of the ATPase VCP/p97 induce cancer cell death
Magnaghi P, D’Alessio R, Valsasina B, Avanzi N, Rizzi S, Asa D, Gasparri F, Cozzi L, Cucchi U, Orrenius C, Polucci P, Ballinari D, Perrera C, Leone A, Galvani A, Donati D, O'Brien T, Jackson P, Isacchi A
Nature Chem Biol (2013), 9, 548–556
View abstract on PubMed

The Polo-Like Kinase 1

NMS-E973, a Novel Synthetic Inhibitor of Hsp90 with Activity against Multiple Models of Drug Resistance to Targeted Agents, Including Intracranial Metastases
Fogliatto G, Gianellini L, Brasca MG, Casale E, Ballinari D, Ciomei M, Degrassi A, De Ponti A, Germani M, Guanci M, Paolucci M, Polucci P, Russo M, Sola F, Valsasina B, Visco C, Zuccotto F, Donati D, Felder ER, Pesenti E, Galvani A, Mantegani S, Isacchi A.
Clin Cancer Res. (2013), 19(13), 3520-32
View abstract on PubMed

The Polo-Like Kinase 1

The Polo-Like Kinase 1 (PLK1) Inhibitor NMS-P937 Is Effective in a New Model of Disseminated Primary CD56(+) Acute Monoblastic Leukaemia.
Casolaro A, Golay J, Albanese C, Ceruti R, Patton V, Cribioli S, Pezzoni A, Losa M, Texido G, Giussani U, Marchesi F, Amboldi N, Valsasina B, Bungaro S, Cazzaniga G, Rambaldi A, Introna M, Pesenti E, Alzani R.
PLoS One. (2013), 8(3), e58424
View abstract on PubMed

PARP inhibitors in cancer therapy

PARP inhibitors in cancer therapy: an update
Papeo G, Casale E, Montagnoli A, Cirla A
Expert Opin Ther Pat. (2013), 23(4), 503-14
View abstract on PubMed

Alkylsulfanyl-1,2,4-triazoles

Alkylsulfanyl-1,2,4-triazoles, a New Class of Allosteric Valosine Containing Protein Inhibitors. Synthesis and Structure-Activity Relationships
Polucci P, Magnaghi P, Angiolini M, Asa D, Avanzi N, Badari A, Bertrand J, Casale E, Cauteruccio S, Cirla A, Cozzi L, Galvani A, Jackson PK, Liu Y, Magnuson S, Malgesini B, Nuvoloni S, Orrenius C, Sirtori FR, Riceputi L, Rizzi S, Trucchi B, O'Brien T, Isacchi A, Donati D, D'Alessio R
J Med Chem (2013) 56(2), 437-450
View abstract on PubMed

RET inhibition: implications in cancer therapy

RET inhibition: implications in cancer therapy
Borrello MG, Ardini E, Locati LD, Greco A, Licitra L, Pierotti MA
Expert Opin Ther Targets (2013), 17(4), 403-19
View abstract on PubMed

Cell line identity finding by fingerprinting

Cell line identity finding by fingerprinting, an optimized resource for short tandem repeat profile authentication
Somaschini A, Amboldi N, Nuzzo A, Scacheri E, Ukmar G, Ballinari D, Malyszko J, Raddrizzani L, Landonio A, Gasparri F, Galvani A, Isacchi A, Bosotti R
Genet Test Mol Biomarkers, (2013), 17(3), 254-9
View abstract on PubMed

In Vivo Target Validation

In Vivo Target Validation by Inducible RNAi in Human Xenograft Mouse Models
Mazzoletti M, Texido G
Methods Mol Biol (2013), 986, 325-37
View abstract on PubMed

Genetically engineered animal models for in vivo target identification

Genetically engineered animal models for in vivo target identification and validation in oncology
Texido G
Methods Mol Biol (2013), (986), 281-305
View abstract on PubMed

Antitumor efficacy on glioma models of PHA-848125

Antitumor efficacy on glioma models of PHA-848125, a multikinase inhibitor able to cross the blood brain barrier
Albanese C, Alzani R, Amboldi N, Degrassi A, Festuccia C, Fiorentini F, Gravina GL, Mercurio C, Pastori W, Brasca MG, Pesenti E, Galvani A, Ciomei M
Br J Pharmacol. (2013), 169(1), 156-66
View abstract on PubMed

Archive 2012

Phase I study of the safety, tolerability and pharmacokinetics of PHA-848125AC, a dual tropomyosin receptor kinase A and cyclin-dependent kinase inhibitor, in patients with advanced solid malignancies
Weiss GJ, Hidalgo M, Borad MJ, Laheru D, Tibes R, Ramanathan RK, Blaydorn L, Jameson G, Jimeno A, Isaacs JD, Scaburri A, Pacciarini MA, Fiorentini F, Ciomei M, Von Hoff DD
Invest New Drugs (2012) 30(6), 2334-2343

The interaction of nemorubicin metabolite PNU-159682 with DNA fragments d(CGTACG)(2), d(CGATCG)(2) and d(CGCGCG)(2) shows a strong but reversible binding to G:C base pairs
Mazzini S, Scaglioni L, Mondelli R, Caruso M, Sirtori FR
Bioorg Med Chem (2012), 20(24),6979-6988

Targeting aurora kinases with danusertib (PHA-739358) inhibits growth of liver metastases from gastroenteropancreatic neuroendocrine tumors in an orthotopic xenograft model
Fraedrich K, Schrader J, Ittrich H, Keller G, Gontarewicz A, Matzat V, Kromminga A, Pace A, Moll J, Bläker M, Lohse AW, Hörsch D, Brümmendorf TH, Benten D
Clin Cancer Res (2012), 18(17), 4621-4632

Down-regulation of the PTTG1 proto-oncogene contributes to the melanoma suppressive effects of the cyclin-dependent kinase inhibitor PHA-848125
Caporali S, Alvino E, Levati L, Esposito AI, Ciomei M, Brasca MG, Del Bufalo D, Desideri M, Bonmassar E, Pfeffer U, D'Atri S
Biochem Pharmacol (2012) Jun 13. [Epub ahead of print]

Cisplatin plus paclitaxel and maintenance of bevacizumab on tumour progression, dissemination, and survival of ovarian carcinoma xenograft models
Oliva P, Decio A, Castiglioni V, Bassi A, Pesenti E, Cesca M, Scanziani E, Belotti D, Giavazzi R
Br J Cancer
(2012), 107(2), 360-369

Identification of a phenylacylsulfonamide series of dual Bcl-2/Bcl-xL antagonists
Perez HL, Banfi P, Bertrand J, Cai ZW, Grebinski JW, Kim K, Lippy J, Modugno M, Naglich J, Schmidt RJ, Tebben A, Vianello P, Wei DD, Zhang L, Galvani A, Lombardo LJ, Borzilleri RM
Bioorg Med Chem Lett
(2012), 22(12), 3946-3950

Pyrazole and pyrimidine phenylacylsulfonamides as dual Bcl-2/Bcl-xL antagonists
Schroeder GM, Wei D, Banfi P, Cai ZW, Lippy J, Menichincheri M, Modugno M, Naglich J, Penhallow B, Perez HL, Sack J, Schmidt RJ, Tebben A, Yan C, Zhang L, Galvani A, Lombardo LJ, Borzilleri RM
Bioorg Med Chem Lett
(2012), 22(12), 3951-3956

Alk inhibitors, a Pharmaceutical Perspective
Ardini E, Galvani A
Front Oncol
(2012), 2(17), 1-8

Development of Biochemical Assays for the Identification of eIF4E-Specific Inhibitors
Visco C, Perrera C, Thieffine S, Sirtori FR, D'Alessio R, Magnaghi P
J Biomol Screen
(2012), 17(5), 581-92

Molecular Recognition of T:G Mismatched Base Pairs in DNA as Studied by Electrospray Ionization Mass Spectrometry.
Riccardi Sirtori F, Aldini G, Colombo M, Colombo N, Malyszko J, Vistoli G, D'Alessio R
ChemMedChem.
(2012), 7(6), 1112-22

Transcriptional analysis of the Aurora inhibitor Danusertib leading to biomarker identification in TP53 wild type cells
Bosotti R, Carpinelli P, Healy S, Locatelli G, Cappella P, Lanfrancone L, Calogero R, Moll J, Isacchi A.
Gene
(2012), 494(2), 202-8

In Vivo Imaging of Lymph Node Migration of MNP- and (111)In-Labeled Dendritic Cells in a Transgenic Mouse Model of Breast Cancer (MMTV-Ras)
Martelli C, Borelli M, Ottobrini L, Rainone V, Degrassi A, Russo M, Gianelli U, Bosari S, Fiorini C, Trabattoni D, Clerici M, Lucignani G
Mol Imaging Biol
(2012), 14(29), 183-96

NMS-P937, an orally available, specific, small molecule Polo-Like Kinase 1 inhibitor with antitumor activity in solid and haematological malignancies
Valsasina B, Beria I, Alli C, Alzani R, Avanzi N, Ballinari D, Cappella P, Caruso M, Casolaro A, Ciavolella A, Cucchi U, De Ponti A, Felder E, Fiorentini F, Galvani A, Gianellini LM, Giorgini ML, Isacchi A, Lansen J, Pesenti E, Rizzi S, Rocchetti M, Sola F, Moll J
Mol Cancer Ther.
(2012), 11(4), 1006-1016

The generation of purinome-targeted libraries as a means to diversify ATP-mimetic chemical classes for lead finding
Felder ER, Badari A, Disingrini T, Mantegani S, Orrenius C, Avanzi N, Isacchi A, Salom B
Mol Divers.
(2012), 16(1), 21-51

5-(2-Amino-pyrimidin-4-yl)-1H-pyrrole and 2-(2-amino-pyrimidin-4-yl)-1,5,6,7-tetrahydro–pyrrolo[3,2-c]pyridin-4-one derivatives as new classes of selective and orally available Polo-like kinase 1 inhibitors
Beria I, Caruso M, Valsasina B,  Ballinari D, Bertrand J, Brasca MB,  Caldarelli M, Cappella P, Fiorentini F,  Gianellini L, Scolaro A
Bioorganic & Medicinal Chemistry Letters
(2012), 22(1), 96-101

Labeling Protocols for In Vivo Tracking of Human Skeletal Muscle Cells (HSkMCs) by Magnetic Resonance and Bioluminescence Imaging
Libani IV, Lucignani G, Gianelli U, Degrassi A, Russo M, Bosari S, Clerici M, Ottobrini L.
Mol Imaging Biol.
(2012), 14(1), 47-59

Archive 2011

  • Summarizing probe intensities of affymetrix GeneChip 3' expression array taking into account day-to-day variability
    Magni P, Simeone A, Healy S, Isacchi A, Bosotti R
    IEEE/ACM Trans Comput Biol Bioinform
    (2011), 8(5), 1425-30
  • A first in man, phase I dose-escalation study of PHA-793887, an inhibitor of multiple cyclin-dependent kinases (CDK2, 1 and 4) reveals unexpected hepatotoxicity in patients with solid tumors
    Massard C, Soria JC, Anthoney DA, Proctor A, Scaburri A, Pacciarini MA, Laffranchi B, Pellizzoni C, Kroemer G, Armand JP, Balheda R, Twelves CJ
    Cell Cycle
    (2011), 10(6), 963-970
  • Influence of pharmacogenetic variability on the pharmacokinetics and toxicity of the aurora kinase inhibitor danusertib
    Steeghs N, Mathijssen RH, Wessels JA, de Graan AJ, van der Straaten T, Mariani M, Laffranchi B, Comis S, de Jonge MJ, Gelderblom H, Guchelaar HJ
    Invest New Drugs
    (2011), 29(5), 953-62
  • Abcg2 overexpression represents a novel mechanism for acquired resistance to the multi-kinase inhibitor Danusertib in BCR-ABL-positive cells in vitro
    Balabanov S, Gontarewicz A, Keller G, Raddrizzani L, Braig M, Bosotti R, Moll J, Jost E, Barett C, Rohe I, Bokemeyer C, Holyoake TL, Brümmendorf TH
    PLoS One
    (2011), 6(4), e19164
  • Mechanisms of Action of a Dual Cdc7/Cdk9 Kinase Inhibitor against Quiescent and Proliferating CLL Cells
    Natoni A, Murillo LS, Kliszczak AE, Catherwood MA, Montagnoli A, Samali A, O'Dwyer M, Santocanale C
    Mol Cancer Ther
    (2011) 10(9), 1624-1634
  • Structural basis for CARM1 inhibition by indole and pyrazole inhibitors
    Sack JS, Thieffine S, Bandiera T, Fasolini M, Duke GJ, Jayaraman L, Kish KF, Klei HE, Purandare AV, Rosettani P, Troiani S, Xie D, Bertrand JA.
    Biochem J.
    (2011) 436(2), 331-339
  • Identification of candidate substrates for poly(ADP-ribose) polymerase-2 (PARP2) in the absence of DNA damage using high-density protein microarrays
    Troiani S, Lupi R, Perego R, Re Depaolini S, Thieffine S, Bosotti R, Rusconi L.
    FEBS J
    (2011) 278(19), 3676-3687
  • Targeting the DFG-in kinase conformation: a new trend emerging from a patent analysis
    Angiolini M
    Future Med Chem.
    (2011) 3(3), 309-337
  • NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor
    Beria I, Bossi RT, Brasca MG, Caruso M, Ceccarelli W, Fachin G, Fasolini M, Forte B, Fiorentini F, Pesenti E, Pezzetta D, Posteri H, Scolaro A, Re Depaolini S, Valsasina B
    Bioorg Med Chem Lett.
    (2011) 21(10), 2969-2974.
  • Targeting aneuploid cancer cells
    Colombo R, Moll J
    Expert Opin Ther Targets
    (2011) 15(5), 595-608
  • From polymer to small organic molecules: a tight relationship between radical chemistry and solid-phase organic synthesis
    Mirizzi D, Pulici M
    Molecules
    (2011) 16(4), 3252-3314
  • Synthesis and SAR of new pyrazolo[4,3-h]quinazoline-3-carboxamide derivatives as potent and selective MPS1 kinase inhibitors
    Caldarelli M, Angiolini M, Disingrini T, Donati D, Guanci M, Nuvoloni S, Posteri H, Quartieri F, Silvagni M, Colombo R
    Bioorg Med Chem Lett.
    (2011) 21(15), 4507-4511

Archive 2010

  • Targeting cell division cycle 7 kinase: a new approach for cancer therapy
    Montagnoli A, Moll J, Colotta F
    Clin Cancer Res.
    (2010), 4503-4508
  • Discovery of drug mode of action and drug repositioning from transcriptional responses
    Iorio F, Bosotti R, Scacheri E, Belcastro V, Mithbaokar P, Ferriero R, Murino L, Tagliaferri R, Brunetti-Pierri N, Isacchi A, di Bernardo D
    Proc Natl Acad Sci
    (2010), 107(33), 14621-6
  • Dual targeting of CDK and tropomyosin receptor kinase families by the oral inhibitor PHA-848125, an agent with broad-spectrum antitumor efficacy
    Albanese C, Alzani R, Amboldi N, Avanzi N, Ballinari D, Brasca MG, Festuccia C, Fiorentini F, Locatelli G, Pastori W, Patton V, Roletto F, Colotta F, Galvani A, Isacchi A, Moll J, Pesenti E, Mercurio C, Ciomei M
    Mol Cancer Ther
    (2010), 2243-2254
  • Crystal structures of anaplastic lymphoma kinase in complex with ATP competitive inhibitors
    Bossi RT, Saccardo MB, Ardini E, Menichincheri M, Rusconi L, Magnaghi P, Orsini P, Avanzi N, Borgia AL, Nesi M, Bandiera T, Fogliatto G, Bertrand JA
    Biochemistry
    (2010), 6813-6825
  • Cell-based assays--Informa Life Sciences' Fifth Annual Conference--Cell-based assays for compound screening and 3D assays
    Gasparri F
    IDrugs
    (2010), 520-522
  • Cell-based assays--Informa Life Sciences' Fifth Annual Conference--Label-free cell-based assays and high-content analysis in drug discovery
    Gasparri F
    IDrugs
    (2010), 523-526
  • Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity
    Bindi S, Fancelli D, Alli C, Berta D, Bertrand JA, Cameron AD, Cappella P, Carpinelli P, Cervi G, Croci V, D'Anello M, Forte B, Giorgini ML, Marsiglio A, Moll J, Pesenti E, Pittalà V, Pulici M, Riccardi-Sirtori F, Roletto F, Soncini C et al
    Bioorg Med Chem.
    2010), 7113-7120.
  • Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding
    Menichincheri M, Albanese C, Alli C, Ballinari D, Bargiotti A, Caldarelli M, Ciavolella A, Cirla A, Colombo M, Colotta F, Croci V, D'Alessio R, D'Anello M, Ermoli A, Fiorentini F, Forte B, Galvani A, Giordano P, Isacchi A, Martina K et al.
    J Med Chem.
    (2010), 7296-7315
  • 4,5-Dihydro-1H-pyrazolo[4,3-h]quinazolines as potent and selective Polo-like kinase 1 (PLK1) inhibitors
    Beria I, Valsasina B, Brasca MG, Ceccarelli W, Colombo M, Cribioli S, Fachin G, Ferguson RD, Fiorentini F, Gianellini LM, Giorgini ML, Moll JK, Posteri H, Pezzetta D, Roletto F, Sola F, Tesei D, Caruso M.
    Bioorg Med Chem Lett.
    (2010), 6489-6494
  • Anaplastic Lymphoma Kinase: role in specific tumours, and development of small molecule inhibitors for cancer therapy
    Ardini E, Magnaghi P, Orsini P, Galvani A, Menichincheri M.
    Cancer Lett.
    (2010), 81-94
  • Targeting the mitotic checkpoint for cancer therapy with NMS-P715, an inhibitor of MPS1 kinase
    Colombo R, Caldarelli M, Mennecozzi M, Giorgini ML, Sola F, Cappella P, Perrera C, Depaolini SR, Rusconi L, Cucchi U, Avanzi N, Bertrand JA, Bossi RT, Pesenti E, Galvani A, Isacchi A, Colotta F, Donati D, Moll J.
    Cancer Res.
    (2010), 10255-10264
  • Phosphorylation of TCTP as a Marker for Polo-like Kinase-1 Activity In Vivo
    Cucchi U, Gianellini LM, DE Ponti A, Sola F, Alzani R, Patton V, Pezzoni A, Troiani S, Saccardo MB, Rizzi S, Giorgini ML, Cappella P, Beria I, Valsasina B.
    Anticancer Res.
    (2010) 30(12), 4973-4985
  • Development of an automated modular system for the synthesis of [11C]acetate
    Felicini C, Någren K, Berton A, Pascali G, Salvadori PA.
    Nucl Med Commun.
    (2010) 1033-1039
  • Destabilizing Aneuploidy by Targeting Cell Cycle and Mitotic Checkpoint Proteins in Cancer Cells.
    Colombo R, Moll J
    Curr Drug Targets
    (2010) 11(10), 1325-1335
  • Targeting Genetic Instability in Cancer Cells
    Colotta F
    Curr Drug Targets
    (2010) 11(10), 1293-1295
  • Miniaturizing bromodeoxyuridine incorporation enables the usage of flow cytometry for cell cycle analysis of adherent tissue culture cells for high throughput screening
    Cappella P, Giorgini ML, Ernestina Re C, Ubezio P, Ciomei M, Moll J.
    Cytometry A
    (2010) 77(10), 953-961
  • Down-regulation of the nucleotide excision repair gene XPG as a new mechanism of drug resistance in human and murine cancer cells
    Sabatino MA, Marabese M, Ganzinelli M, Caiola E, Geroni C, Broggini M.
    Mol Cancer
    (2010) 24(9), 259
  • Structure-based optimization of PDK1 inhibitors
    Angiolini M, Banfi P, Casale E, Casuscelli F, Fiorelli C, Silvagni M, Zuccotto F, Saccardo MB
    Bioorganic & Med Chem Lett
    (2010) 4095-4099
  • Identification of Potent Pyrazolo[4,3-h]quinazoline-3-carboxamides as Multi-Cyclin-Dependent Kinase Inhibitors
    Traquandi G, Ciomei M, Ballinari D, Casale E, Colombo N, Croci V, Fiorentini F, Isacchi A, Longo A, Mercurio C, Panzeri A, Pastori W, Pevarello P, Volpi D, Roussel P, Vulpetti A, Brasca MG
    J Med Chem
    (2010) 53, 2171-2187
  • Role of glutathione transferases in the mechanism of Brostallicin activation
    Pezzola S, Antonini G, Geroni C, Beria I, Colombo M, Broggini M, Mongelli N, Leboffe L, MacArthur R, Mozzi AF, Federici G, Caccuri AM
    Biochemistry
    (2010) 49, 226-235
  • Therapeutic efficacy of the pan-cdk inhibitor PHA-793887 in vitro and in vivo in engrafment and high-burden leukemia models
    Alzani R, Pedrini O, Albanese C, Ceruti R, Casolaro A, Patton V, Colotta F, Rambaldi A, Introna M, Pesenti E, Ciomei M, Golay J
    Experimental Hematology
    (2010) 38, 259-269
  • Phase I dose-escalation study of brostallicin, a minor groove binder, in combination with cisplatin in patients with advanced solid tumors
    Caponigro F, Lorusso D, Fornari G, Barone C, Merlano M, Airoldi M, Schena M, MacArthur R, Weitman S, Jannuzzo MG, Crippa S, Fiorentini F, Petroccione A, Comis S
    Cancer Chemother Pharmacol
    (2010) 66(2), 389-64
  • Efficacy of PHA-848125, a Cyclin Dependent Kinase inhibitor, on the K-RasG12DLA2 lung adenocarcinoma transgenic mouse model: evaluation by multimodality imaging
    Degrassi A, Russo M, Nanni C, Patton V, Alzani R, Giusti A, Fanti S, Ciomei M, Pesenti E, Texido G
    Mol Cancer Ther
    (2010) 9(3), 673-681
  • Optimisation of 6,6-Dimethyl Pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a Potent CDK Inhibitor Suitable for Intravenous Dosing
    Brasca MG, Albanese C, Alzani R, Amici R, Avanzi N, Ballinari D, Bischoff J, Borghi D, Casale E, Croci V, Fiorentini F, Isacchi A, Mercurio C, Nesi M, Orsini P, Pastori W, Pesenti E, Pevarello P, Roussel P, Varasi M, Volpi D, Vulpetti A, Ciomei M
    Bioorganic & Medicical Chemistry
    (2010) 18, 1844-1853
  • Transcriptional analysis of an E2F gene signature as a biomarker of activity of the Cyclin-dependent kinase inhibitor PHA-793887 in tumor and skin biopsies from a phase I clinical study
    Locatelli G, Bosotti R, Ciomei M, Brasca G,Calogero R, Mercurio C, Fiorentini F, Bertolotti M, Scacheri E, Scaburri A, Pesenti E, De Baere T, Soria JC, Lazar V, Isacchi A.
    Mol Cancer Ther
    (2010) 9(5), 1265-1273
  • Identification of Myb-binding protein 1a (MYBBP1A) as a novel substrate for Aurora B kinase
    Perrera C, Colombo R, Valsasina B, Carpinelli P, Troiani S, Modugno M, Gianellini L, Isacchi A, Moll J, Rusconi L
    JBC
    (2010) 285(16), 11775-11785
  • Through the "Gatekeeper Door": Exploiting The Active Kinase Conformation
    Zuccotto F, Ardini E, Casale E, Angiolini M
    J Med Chem
    (2010) 53, 2681-2694
  • The cyclin-dependent kinase inhibitor PHA-848125 suppresses the in vitro growth of human melanomas sensitive or resistant to temozolomide, and shows synergistic effects in combination with this triazene compound
    Caporali S, Alvino E, Starace G, Ciomei M, Brasca M.G, Levati L, Garbin A, Castiglia D, Covaciu C, Bonmassar E, D’Atri S.
    Pharmacol Research
    (2010) 61, 437-448
  • Identification of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline Derivatives as a New Class of Orally and Selective Plk1 Inhibitors
    Beria I, Ballinari D, Bertrand J, Borghi D, Bossi RT, Brasca MG, Cappella P, Caruso M, Ceccarelli W, Ciavolella A, Cinziani C, Croci V, DePonti A, Fachin G, Fergusson RD, Lansen J, Moll JK, Pesenti E, Posteri H, Perego R, Rocchetti M, Storici P et a
    J. Med. Chem.
    (2010) 53, 3532-3551

Archive 2009

  • Identification of N,1,4,4-Tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a Potent, Orally Available Cyclin Dependent Kinase Inhibitor
    Brasca MG, Amboldi A, Ballinari D, Cameron A, Casale E, Cervi G, Colombo M, Colotta F, Croci V, D’Alessio R, Fioentini F, Isacchi A, Mercurio C, Moretti W, Panzeri A, Pastori W, Pevarello P, Quartieri F, Roletto F, Traquandi G, et al.
    J. Med. Chem.
    (2009) 52, 5152-5163
  • A submarine journey: the pyrrole-imidazole alkaloids
    Forte B, Malgesini B, Piutti C, Quartieri F, Scolaro A, Papeo GL
    Marine Drugs
    (2009) 7, 705-753
  • In vitro and in vivo efficacy of 6-(7-nitro-2,1,3-benzoxadiazol-4-ylthio)hexanol (NBDHEX) on human melanoma
    Pellizzari Tregno F, Sau A, Pezzola S, Geroni C, Lapenta C, Spada M, Filomeni G, Bonanno E, Federici G, Caccuri AM
    Eur J of Cancer
    (2009) 45, 2606-2617
  • Testing additivity of anticancer agents in pre-clinical studies: a PK/PD modelling approach
    Rocchetti M, DelBene F, Germani M, Fiorentini F, Poggeti I, Pesenti E, Magni P, DeNicolao G
    Eur J of Cancer
    (2009) 45, 3336-3346
  • A Perl procedure for protein identification by peptide mass fingerprinting
    Tiengo A, Barbarini N, Troiani S, Rusconi L, Magni P
    BMC Bioinformatics
    (2009) 10 (suppl 12) S11
  • Aurora kinase inhibitor PHA-739358 suppresses growth of hepatocellular carcinoma in vitro and in a Xenograft mouse model
    Benten D, Keller G, Quaas A, Schrader J, Gontarewicz A, Balabanov S, Braig M, Wege H, Moll J, Lohse AW, Brummendorf T.
    Neoplasia
    (2009) 11(9), 934-944
  • Diagnostic exercise: sudden death in a mouse with experimentally induced acute myeloid leukemia.
    Radaelli E , Marchesi F, Patton V, Scanziani E
    Vet Pathol.
    (2009) 46(6):1301-5
  • A phase I dose-escalation study of danusertib (PHA-739358) administered as a 24-hour infusion with and without granulocyte colony-stimulating factor in a 14-day cycle in patients with advanced solid tumors.
    Cohen RB, Jones SF, Aggarwal C, von Mehren M, Cheng J, Spigel DR, Greco FA, Mariani M, Rocchetti M, Ceruti R, Comis S, Laffranchi B, Moll J, Burris HA.
    Clin Cancer Res.
    (2009) 15(21):6694-701
  • Thymidine kinase 1 expression defines an activated G1 state of the cell cycle as revealed with site-specific antibodies and ArrayScan assays.
    Gasparri F, Wang N, Skog S, Galvani A, Eriksson S.
    Eur J Cell Biol.
    (2009) 88(12):779-85
  • Poly(ADP-ribose) polymerase ibhibition in cancer therapy: Are we close to maturity?
    Papeo GL, Forte B, Orsini P, Perrera C, Posteri H, Scolaro A, Montagnoli A
    Expert Opinion Therapeutic Patents
    (2009) 19(10), 1377-1400
  • Optimization of pyrazole inhibitors of coactivator associated arginine methyltransferase 1 (CARM1)
    Huynh T, Chen Z, Pang S, Geng J, Bandiera T, Bindi S, Vianello P, Roletto F, Thieffine S, Galvani A, Vaccaro W, Poss M, Trainor G, Lorenzi M, Gottardis M, Jayaraman L, Purandare A
    Bioorganic & Medicinal Chemistry Letters
    (2009) 9(11), 2924-2927
  • Phase I Pharmacokinetic and Pharmacodynamic Study of the Aurora Kinase Inhibitor Danusertib in Patients with Advanced or Metastatic Solid Tumors
    Steeghs N, Eskens FALM, Gelderblom H, Verweij J, Nortier JWR, Ouwerkerk J, Noort C , Mariani M, Spinelli R, Carpinelli P, Laffranchi B, de Jonge M.
    Journal Clinical Oncology
    (2009) 27(30), 5094-5101
  • Cell division cycle 7 kinase inhibitors: 1H-pyrrolo[2,3-b]pyridines, synthesis and structure-activity relationships
    Ermoli A, Bargiotti A, Brasca MG, Ciavolella A, Colombo N, Fachin G, Isacchi A, Menichincheri M, Molinari A, Montagnoli A, Pillan A, Rainoldi S, Sirtori FR, Sola F, Thieffine S, Tibolla M, Valsasina B, Volpi D, Santocanale C, Vanotti E
    Journal of Medicinal Chemistry
    (2009) 52(14), 4380-4390
  • First Cdc7 kinase inhibitors: pyrrolopyridinones as potent and orally active antitumor agents. 2. Lead discovery
    Menichincheri M et al.
    Chem Med Chem
    (2009) 52(2), 293-307
  • Design, synthesis, and biological evaluation of levoglucosenone-derived ras activation inhibitors
    Müller C, Gomez-Zurita Frau MA, Ballinari D, Colombo S, Bitto A, Martegani E, Airoldi C, van Neuren AS, Stein M, Weiser J, Battistini C, Peri
    Chem Med Chem
    (2009) (4), 524-528
  • Immunohistopathological and neuroimaging characterization of murine orthotopic xenograft models of glioblastoma multiforme recapitulating the most salient features of human disease
    Radaelli E, Ceruti R, Patton V, Russo M, Degrassi A, Croci V, Caprera F, Stortini G, Scanziani E, Pesenti E, Alzani R
    Histology and Histopathology
    (2009) 24(7), 879-891
  • Cancer-related inflammation, the seventh hallmark of cancer: links to genetic instability
    Colotta F, Allavena P, Sica A, Garlanda C, Mantovani A.
    Carcinogenesis
    (2009) 30(7), 1073-1081
  • A straightforward total synthesis of (-)-chaetominine
    Malgesini B, Forte B, Borghi D, Quartieri F, Papeo G, Gennari C
    Chemistry: a European Journal
    (2009) 15(32), 7922-7929
  • Is there a future for Aurora kinase inhibitors for anticancer therapy?
    Carpinelli P, Moll J
    Curr Opin Drug Discov Devel
    (2009) 12(4), 533-542
  • Highly efficient synthesis of 5-benzyl substituted 3-aminoindazoles
    Orsini P, Menichincheri M, Vanotti E, Panzeri A
    Tetrahedron letters
    (2009) 50, 3098-3100
  • First Cdc7 Kinase Inhibitors: Pyrrolopyridinones as Potent and Orally Active Antitumor Agents. 2. Lead Finding
    Menichincheri M, Bargiotti A, Bossi R, Cirla A, D’Alessio R, Forte B, Martina K, Orsini P, Orzi F, Pillan A, Scolaro A, Tibolla M, Varasi M, Vanotti E et al.
    Journal of Medicinal Chemistry
    (2009) 52 (2), 293-307
  • Cancer-associated stroma affects FDG uptake in experimental carcinomas. Implications for FDG-PET delineation of radiotherapy target
    Farace P, D'Ambrosio D, Merigo F, Galliè M, Nanni C, Spinelli A, Fanti S, Degrassi A, Sbarbati A, Rubello D, Marzola P
    Eur J Nucl Med Mol Imaging
    (2009) 36(4), 616-623
  • Stereoselective Synthesis of (Z)-Axino- and (Z)-Debromoaxinohydantoin
    Tutino F, Posteri H, Borghi D, Quartieri F, Mongelli N, Papeo G
    Tetrahedron
    (2009) 65, 2372-2376
  • Improved Synthesis of Polyfluorinated L-lysine for 19F NMR-Based Screening
    Malgesini B, Felder E, Mongelli N, Papeo G
    Mol. Divers
    (2009) 13, 53-56
  • Estrogen Suppression in premenopausal women following 8 weeks of treatment with exemestane and triptorelin versus triptorelin alone
    Jannuzzo MG, DiSalle E, Spinelli R, Pirotta N, Buchan P, Bello A
    Breast Cancer Res Treat
    (2009) 113(3), 491-499

Archive 2008

  • The structure of P-TEFb (CDK9/cyclin T1), its complex with flavopiridol and regulation by phosphorylation
    Baumli S, Lolli G, Lowe ED, Troiani S, Rusconi L, Bullock AN, Debreczeni JE, Knapp S, Johnson LN
    EMBO Journal
    (2008) 27, 1907-1918
  • PHA-680626 exhibits anti-proliferative and pro-apoptotic activity on Imatinib-resistant chronic myeloid leukemia cell lines and primary CD34+ cells by inhibition of both Bcr-Abl tyrosine kinase and Aurora kinases
    Gontarewicz A, Balabanov S, Keller G, Panse J, Schafhausen P, Bokemeyer C, Fiedler W, Moll J, Brümmendorf TH
    Blood
    (2008) 32(12), 1857-1865
  • Target validation and biomarker identification in Oncology; The example of Aurora kinases. Target validation to biomarker development; Focus on RNA interference.
    Colombo R, Moll J
    Molecular Diagnosis & Therapy
    2008 (12), 63-60 & 71-76
  • Chapter 12. Basic Approaches to Gene/Exon Level Data Analysis: 3'IVT and Exon 1.0 ST Microarray Platforms
    Bosotti R, Marchesi V, Calogero R
    Chapter for a Book entitled: “Oligonucleotide Array Sequence Analysis” edited by Novascience
    (2008) 12, 347-366
  • In vitro hepatic conversion of the anticancer agent nemorubicin to its active metabolite PNU-159682 in mice, rats and dogs: a comparison with human liver microsomes
    Quintieri L, Fantin M, Palatini P, De Martin S, Rosato A, Caruso M, Geroni C, Floreani M.
    Biochemical Pharmacology
    (2008) 76(6), 784-795
  • Cell proliferation method: click chemistry-based by BrdU coupling for multiplex antibody staining
    Cappella P, Gasparri F, Pulici M, Moll J
    Book Chapter "Current Protocols of Cytometry"
    (2008) suppl 45, unit 7.34
    Abstract
  • High-content analysis of kinase activity in cells
    Gasparri F, Sola F, Bandiera T, Moll J, Galvani A
    Combinatorial Chemistry & High Throughput Screening
    (2008) 11, 523-536
  • A novel method based on click chemistry, which overcomes limitations of cell cycle analysis by classical determination of BrdU incorporation, allowing multiplex antibody staining
    Cappella P, Gasparri F, Pulici M, Moll J
    Cytometry
    (2008) 73 (7), 623-636
  • Occurrence and Modality of the Interaction between Brostallicin and the Human Glutathione S-transferases GSTP1-1 and GSTM2-2
    Pezzola S, Turella P, Geroni C, Beria I, Colombo M, Mongelli N, Ricci G, MacArthur R, Federici G, Caccuri AM
    J Biol Chem
  • Aurora kinase inhibitors: identification and preclinical validation of their biomarkers
    Carpinelli P, Moll J
    Expert Opin Ther Targets
    (2008), 12 (1), 69-80
    Abstract
  • A Ccd7 kinase inhibitor restricts initiation of DNA replication ad has antitumor activity
    Montagnoli A, Valsasina B, Menichincheri M, Croci V, Tibolla M, Tenca PL, Rainoldi S, Brotherton D, Albanese C, Patton V, Alzani R, Ciavolella A, Sola F, Molinari A, Volpi D, Bensimon A, Vanotti E, Santocanale C
    Nature Chemical Biology
    (2008) 4 (6), 357-365
    Abstract
  • NICOTINOYL AZIDE
    Papeo GL, Posteri H, Vianello P, Varasi M
    E.R.O.S. Encyclopedia of Reagents for Organic Synthesis
    (2008), 1-6
  • First Cdc7 Kinase Inhibitors: Pyrrolopyridinones as Antitumor Agents. 1. Synthesis and Structure-Activity Relationships
    Vanotti E, Amici R, Bargiotti A, Berthelsen J, Bosotti R, Ciavolella A, Cirla A, Cristiani C, D’Alessio R, Forte B, Martina K, Menichincheri M, Molinari A, Montagnoli A, Orsini P, Pillan A, Roletto F, Scolaro A, et al.
    Journal of Medicinal Chemistry
    (2008) 51, 487-501
    Abstract
  • Simultaneous targeting of Aurora kinases and Bcr-Abl kinase by the small molecule inhibitor PHA-739358 is effective against imatinib-resistant BCR-ABL mutations including T315I
    Brummendorf T J. Moll
    Blood
    (2008) 111(8), 4355-4364

Archive 2007

  • Regioselective g-alkylation of tert-butyl 2,4-dioxopiperidine-1-carboxylate
    Orsini P, Maccario A, Colombo N
    Synthesis
    (2007) 20, 3185-3190
  • Anticancer Drug Discovery and Development
    Colotta F
    Chapter of book: Targeted Therapies in cancer. Myth or Reality?
    (2007) 610, 19-41
  • Aurora kinases and their inhibitors: more than one target and one drug
    Carpinelli P, Moll J
    Chapter of book: Targeted Therapies in cancer. Myth or Reality?
    (2007) 610, 54-73
  • Crystal structure of the T315I Abl mutant in complex with the aurora kinases inhibitor PHA-739358.
    Modugno M, Casale E, Soncini C, Rosettani P, Colombo R, Lupi R, Rusconi L, Fancelli D, Carpinelli P, Cameron AD, Isacchi A, Moll J.
    Cancer Research
    (2007) 67 (17):7987-90.
  • PHA-739358, a potent inhibitor of Aurora kinases with a selective target inhibition profile relevant to cancer
    Carpinelli P, Ceruti R, Giorgini ML, Cappella P, Gianellini L, Croci V, Degrassi A, Texido G, Rocchetti M, Vianello P, Rusconi L, Storici P, Zugnoni P, Arrigoni C, Soncini C, Alli C, Patton V, Marsiglio A, Ballinari D, Pesenti E, Fancelli D, Moll J.
    Mol Cancer Ther.
    2007 6 (12):3158-68
  • Development and Validation of In Silico Models for Estimating Drug Preformulation Risk in PEG400/Water and Tween80/Water Systems.
    Crivori P, Morelli A, Pezzetta D, Poggesi I, Rocchetti M.
    European J of Pharmaceutical Sciences
    (2007), 32 (3):169-181
    Abstract
  • Pyrazoles as efficient adenine-mimetic heterocycles for the discovery CDK inhibitors
    Pevarello P, Vulpetti A
    Inhibitors of cyclin-dependent kinases as anti-tumor agents (Book)
    (2007) 15, 323-347
    Abstract
  • Cell-cycle inhibitor profiling by high-content analysis
    Gasparri F, Ciavolella A, Galvani A
    Advances in Molecular Oncology (Book)
    (2007) 604, 137-148
    Abstract
  • 6-Substituted Pyrrolo[3,4-c]pyrazoles: An Improved Class of CDK2 Inhibitors
    Brasca MG, Albanese C, Amici R, Ballinari D, Corti L, Croci V, Fancelli D, Fiorentini F, Nesi M, Orsini P, Orzi F, Pastori W, Perrone P, Pesenti E, Pevarello P, Riccardi-Sirtori F, Roletto F, Roussel P, Varasi M, Vulpetti A, Mercurio C
    ChemMedChem
    (2007), 2, 841-852
    Abstract
  • Cross platform microarray analysis for robust identification of differentially expressed genes
    Bosotti R, Locatelli G, Healy S, Scacheri E, Sartori L, Mercurio C, Calogero R and Isacchi A
    BMC Bioinformatics
    (2007) 8, S5
    Abstract
  • Magnetic Resonance Imaging and Histopathological Characterization of Prostate Tumors in TRAMP Mice as Model for Pre-Clinical Trials
    De Grassi A, Russo M, Scanziani E, Giusti A, Ceruti R, Texido G, Pesenti E
    The prostate
    (2007) 67,396-404
    Abstract
  • Antitumor Activity of Edotecarin in Breast Carcinoma Models
    Ciomei M, Croci V, Stellari F, Amboldi N, Giavarini R, Pesenti E
    Cancer Chemotherapy and Pharmacology
    (2007) 60, 2, 229-235
    Abstract
  • Structures of the human eIF4E homologous protein, 4EHP, in its m(7)GTP-bound and Unliganded Forms
    Rosettani P, Knapp S, Vismara S, Rusconi MG, Cameron A
    Journal of Molecular Biology
    (2007) 368, 3, 691-705
    Summary
  • Poly-Fluorinated Amino acids for Sensitive 19F NMR-Based Screening and Kinetic Measurements
    Papeo GL, Giordano P, Brasca MG, Buzzo F, Caronni D, Ciprandi F, Mongelli N, Veronesi M, Vulpetti A, Dalvit C
    J. Am. Chem. Soc.
    (2007), 129 5665-5672
    Abstract
  • Ongoing phase I and II studies of novel anthracyclines
    Sessa C, Valota O, Geroni C
    Cardiovascular Toxicology
    (2007) 7, 75-79
    Conclusion
  • Bortezomib inhibits nuclear factor-kB dependent survival and has potent in vivo activity in mesothelioma
    Sartore-Bianchi A, Gasparri F, Galvani A, Nici L, Darnowski JW, Barbone D, Fennell DA, Gaudino G, Porta C, Mutti L
    Clinical Cancer Research
    (2007) 13, 19, 5942-5951
    Abstract
  • De Novo Synthesis of thiophenes on a polymeric support
    Traversone A, Brill W
    Tetrahedron Letters
    (2007) 48, 3535-3538
    Abstract
  • Assessment of QT Liabilities in Drug Development: Regulatory Status and Current Practices
    Arrigoni C, Crivori P
    Cell Biology and Toxicology
    (2007), 23(1):1-13
    Abstract
  • Synthesis of PHA-690509 labelled with 14C
    Fontana E, Giribone D, Feliciti C
    J of Labelled Compounds and Radiopharm
    (2007), 50:225-227
    Abstract
  • Evaluation of a Physiological-Based Pharmacokinetic Modeling for Simulation of First Time in Animal Study
    Germani M, Crivori P, Rocchetti M, Burton PS, Wilson AGE, Smith ME, Poggesi I
    European J. of Pharmaceutical Sciences
    (2007), 31:190-201
    Abstract
  • Assessing and managing toxicities induced by kinase inhibitors
    Castoldi RE, Pennella G, Saturno GS, Grossi P, Brughera M, Venturi M
    Current Opinion in Drug Discovery & Development
    (2007), 10(1):53-7
    Abstract
  • Predicting the active doses in humans from animal studies: A novel approach in oncology
    Rocchetti M, Simeoni M, Pesenti E, De Nicolao G, Poggesi I
    Eur. J. Can.
    (2007), 43(12):1862-1868
    Abstract
  • Cdc7 is an active kinase in human cancer cells undergoing replication stress
    Tenca P, Brotherton D, Montagnoli A, Rainoldi S, Albanese C, Santocanale C
    Journal of Biological Chemistry
    (2007) 282(1), 208-215
    Abstract

Archive 2006

  • Analysis of brostallicin effect on different human gastrointestinal cancer cell lines
    Scovassi AI, Gorrini C, Pastori W, Ciomei M
    Letters in Drug Design & Discovery
    (2006) 3, 524-527
  • C-C- bond forming reactions
    Brill WK.-D, Papeo G
    Combinatorial Chemistry
    (2006) 26,143-360
  • 3-Amino-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: a new class of CDK2 inhibitors
    Pevarello P, Fancelli D, Vulpetti A, Amici R, Villa M, Pittalà V, Vianello P, Cameron A, Ciomei M, Mercurio C, Bischoff JR, Roletto F, Varasi M and Brasca MG
    Bioorganic and Medicinal Chemistry Letters
    (2006) 16, 1084-1090
  • Compounds and methods for inhibiting mitotic progression
    Fancelli D
    Expert Opin Ther Patents
    (2006) 16(8), 1179-1182
  • 1,4,5,6-Tetrahydropyrrolo [3,4-c]pyrazoles: Identification of a Potent Aurora Kinase Inhibitor with a Favorable Antitumor Kinase Inhibition Profile
    Fancelli D, Moll J, Varasi M, Bravo R, Artico R, Berta D, Bindi S, Cameron A, Candiani I, Cappella P, Carpinelli P, Croci W, Forte B, Giorgini ML, Klapwijk J, Marsiglio A, Pesenti E, Rocchetti M, Roletto F, Severino D, Soncini C, Storici P, Tonani R,
    J Med Chem
    (2006) 49, 7247-7251
  • Bicyclic Carbohydrate-Derived Scaffolds for Combinatorial Libraries
    Cervi G, Peri F, Battistini C, Gennari C, Nicotra
    Bioorganic & Medicinal Chemistry
    (2006), 14, 3349-3367
  • Structure-based Drug Design to the Discovery of New 2-aminothiazole CDK2 Inhibitors
    Vulpetti A, Casale E, Roletto F, Amici R, Villa M, Pevarello P
    Journal of Molecular Graphics and Modelling
    (2006) 24, 341-348
  • Inhibition of Protein-Protein Interactions: The Discovery of Druglike B-Catenin Inhibitors by Combining Virtual and Biophysical Screening
    Trosset J, Dalvit C, Knapp S, Fasolini M, Veronesi M, Mantegani S, Gianellini L, Catana C, Sundström M, Stouten P, Moll J
    Proteins: Structure, Function and Bioinformatics
    (2006) 64, 60-67
  • 1,3,4-Oxadiazole formation as traceless release in solid phase organic synthesis
    Cesarini S, Colombo N, Pulici M, Felder ER and Brill WK-D
    Tetrahedon Letters
    (2006) 62, 10223-10236
  • Multiparametric cell-cycle analysis by automated microscopy
    Gasparri F, Cappella P, Galvani A
    J Biomol Screen
    (2006) 11(6), 586-598
  • NMR-Based Quality Control Approach for Identification of False Positives and False Negatives in High Throughput Screening
    Dalvit C, Caronni D, Mongelli N, Veronesi M, Vulpetti A
    Current Drug Discovery Technologies
    (2006) 3, 115-124
  • PHA-680632, a novel Aurora kinases inhibitor with potent anti-tumoral activity
    Soncini C, Carpinelli P, Gianellini L, Fancelli D, Vianello P, Rusconi L, Storici P, Zugnoni P, Pesenti E, Croci V, Ceruti R, Giorgini ML, Cappella P, Ballinari D, Sola F, Varasi M, Bravo R, Moll J
    Clinical Cancer Research
    (2006) 12(13), 4080-4089
  • Cyclin-Dependent Kinase 2 function in normal DNA repair and is a therapeutic target in BRCA1- deficient Cancers
    Deans AJ, Khanna KK, McNees CJ, Mercurio C, Heierhorst J and McArthur GA
    Cancer Research
    (2006) 66(16), 8219-8226
  • A practical synthesis of the major metabolite of a potent CDK2/cyclin A inhibitor
    Nesi M, Borghi D, Brasca MG, Fiorentini F and Pevarello P
    Bioorganic & Medicinal Chemistry Letters
    (2006) 16, 3205-3208
  • Identification of Mcm2 phosphorylation sites by S-phase regulating kinases
    Montagnoli A, Valsasina B, Brotherton D, Troiani S, Rainoldi S, Tenca PL, Molinari A and Santocanale C
    The Journal of Biological Chemistry
    (2006) 281(5), 10281-10290

Archive 2005

  • Linear and nonlinear methods in modeling the aqueous solubility of organic compounds
    Catana C, Gao H, Orrenius C, Stouten PF
    J. Chem. Inf. Model.
    (2005) 45, 170-176
  • Rapid NMR-based functional screening and IC50 measurements performed at unprecedentedly low enzyme concentration
    Dalvit C, Papeo GL, Mongelli N, Giordano P, Saccardo B, Costa A, Veronesi M, Ko SY
    Drug Dev Res (2005)
    64, 105-113
  • Formation and antitumor activity of PNU-159682, a major metabolite of nemorubicin in human liver microsomes
    Quintieri L, Geroni C, Fantin M, Battaglia R, Rosato A, Speed W, Zanovello P, Floreani M.
    Clinical Cancer Research
    (2005), 11, 1608-1617
  • Total Synthesis of (±)-Cyclooroidin
    Papeo G, Gomez-Zurita Frau MA, Borghi D, Varasi M
    Tetrahedron Letters
    (2005) 46, 8635-8638
  • Solid-phase synthesis of pyrido[2,3-d]pyrimidin-7-ones
    Angiolini M, Fusar Bassini D, Gude M, Menichincheri M
    Tetrahedron Letters
    (2005) 46, 8749-8752
  • A New Glycociamidine Ring Precursor: Synthesis of (Z)-Hymenialdisine, (Z)-2-Debromohymenialdisine and (±)-endo-2-Debrormohyemialdisine
    Papeo G, Posteri H, Borghi B, Varasi M
    Organic Letters
    (2005) 7(25), 5641-5644
  • Sensitivity Improvement in the 19F NMR-based Screening Experiments: Theoretical Considerations and Experimental Applications
    Dalvit C, Mongelli N, Papeo G, Giordano P, Veronesi M, Moskau D, Kümmerle R
    Journal of the American Chemical Society
    (2005) 127, 13380-13385
  • Inhibitors of Aurora kinases for the treatment of cancer
    Fancelli D, Moll J
    Expert Opin Ther Patents
    (2005), 15(9), 1169-1182
  • 4-demethoxy-3'-deamino-3'aziridinyl-4'methylsulphonyl-daunorubicin (PNU-159548): a new promising candidate for chemotherapeutic treatment of osteosarcoma patients
    Pasello M, Hattinger CM, Stoico G, Manara MC, Benini S, Geroni C, Mercuri M, Scotlandi K, Picci P, Serra M
    Eur J Cancer
    (2005) 41, 2184-2195
  • An Analysis of the Binding Modes of ATP-Competitive CDK2 Inhibitors as Revealed by X-Ray Structures of Protein-Inhibitor Complexes
    Vulpetti A, Pevarello P
    Current Medicinal Chemistry-Anti-Cancer Agents
    (2005) 5, 561-573
  • 3-Acylaminopyrazole Derivatives via Regioselectively N-Protected 3-nitropyrazole
    Orsini P, Traquandi G, Sansonna P, Pevarello P
    Tetrahedron Letters
    (2005) 46, 933-935
  • Traceless Solid-Phase Synthesis of 2-Amino-5-alkylidene-thiazol-4-ones
    Pulici M, Quartieri F
    Tetrahedron Letters
    (2005) 46, 2387-2391
  • Benzodipyrazoles: a new class of potent CDK2 inhibitors
    D'Alessio R, Bargiotti A, Betz S, Brasca G, Cameron A, Ermoli A, Marsiglio A, Polucci P, Roletto F, Tibolla M, Vazquez M, Vulpetti A, Pevarello P
    Bioorganic and Medicinal Chemistry Letters
    (2005) 15, 1315-1319
  • Regulation of the Wild-Type and Y1235D Mutant Met Kinase Activation
    Cristiani C, Rusconi L, Perego R, Schiering N, Kalisz H, Knapp S, Isacchi A
    Biochemistry
    (2005) 44, 14110-14119
  • Pyrazolyl-benzoxazole derivatives as protein kinase inhibitors. Design and validation of a combinatorial library
    Berta D, Felder E, Villa M, Vulpetti A
    Tetrahedron Letters
    (2005) 61, 10801-10810
  • Virtual screening to Enrich a Compound Collection with CDK2 inhibitors using Docking, Scoring and Consensus Scoring
    Cotesta S, Giordanetto F, Trosset JY, Crivori P, Kroemer R, Stouten P, Vulpetti A
    Proteins
    (2005) 60, 629-643
  • Searching for biomarkers of Aurora-A kinase activity: Identification of in vitro substrates through a modified KESTREL approach
    Troiani S, Uggeri M, Moll J, Isacchi A, Kalisz HM, Rusconi L, Valsasina B
    Journal of Proteome Research
    (2005) 4, 1296-1303
  • Quantitative NMR in Synthetic and Combinatorial Chemistry
    Rizzo V, Pinciroli V
    Journal of Pharmaceutical & Biomedical Analysis
    (2005) 8(5), 851-857
  • 3-Aminopyrazole inhibitors of CDK2/cyclin A as Antitumor agents. 2. Lead Optimization
    Pevarello P, Brasca MG, Orsini P, Traquandi G, Longo A, Nesi M, Orzi F, Piutti C, Sansonna P, Varasi M, Cameron A, Vulpetti A, Roletto F, Alzani R, Ciomei M, Albanese C, Pastori W, Marsiglio A, Pesenti E, Fiorentini F, Bischoff JR, Mercurio C
    J Med Chem
    (2005) 48, 2944-2956
  • Potent and Selective Aurora-A Inhibitors Identified by the Expansion of a Novel Scaffold for Protein Kinase Inhibition
    Fancelli D, Berta D, Bindi S, Cameron A, Cappella P, Carpinelli P, Catana C, Forte B, Giordano P, Giorgini ML, Mantegani S, Marsiglio A, Meroni M, Moll J, Pittalà V, Roletto F, Severino D, Soncini C, Storici P, Tonani R, Varasi M, Vulpetti A and Vian
    J. Med. Chem.
    (2005), 48, 3080-3084
  • Trifluoroacetic Anhydride-Mediated Solid-Phase Version of the Robinson-Gabriel Synthesis of Oxazoles
    Pulici M, Quartieri F, Felder ER
    J Comb Chem
    (2005) 7, 463-473
  • Structure-based approaches to improve selectivity: CDK2 - GSK3b binding site analysis.
    Vulpetti A, Crivori P, Cameron A, Bertrand J, Brasca G, D'Alessio R, Pevarello P
    J Chem Inf Model
    (2005), 45, 1282-1290
  • PoInTree: a polar and interactive Phylogenetic tree
    Carreras M, Gianti E, Sartori L, Plyte S, Isacchi A, Bosotti R
    Gen Prot Bioinfo
    (2005) 3(1), 58-61
  • Cyclin-dependent kinase (CDK) inhibitors: a survey of the recent patent literature
    Pevarello P, Villa M
    Expert Opin Ther Patents
    (2005) 15 (6), 675-703

Archive 2004

  • Catecholic flavonoids acting as telomerase inhibitors
    Menichincheri M, Ballinari D, Bargiotti A, Bonomini L, Ceccarelli W, D'Alessio R, Fretta A, Moll J, Polucci P, Soncini C, Tibolla M, Trosset JY, Vanotti E.
    J. Med. Chem.
    (2004) 47, 6466-6475
  • The death domain protein p84N5, but not the short isoform p84N5s, is cell cycle-regulated and shuttles between the nucleus and the cytoplasm
    Gasparri F, Sola F, Locatelli G, Muzio M.
    FEBS Letters
    (2004) 574, 13-19
  • Sequence and structural analysis of kinase ATP pocket residues
    Vulpetti A, Bosotti R
    Il Farmaco
    (2004) 10, 759-765
  • Influence of molecular flexibility and polar surface area metrics on oral bioavailability in the rat
    Lu JJ, Crimin K, Goodwin JT, Crivori P, Orrenius C, Xing L, Tandler PJ, Vidmar TJ, Amore BM, Wilson AG, Stouten PF, Burton PS
    J. Med. Chem.
    (2004) 47, 6104-6107
  • Cdc7 inhibition reveals a p53-dependent replication checkpoint that is defective in cancer cells
    Montagnoli A, Tenca P, Sola F, Carpani D, Brotherton D, Albanese C, Santocanale C.
    Cancer Research
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