NMS Company
Publications
Publications
2010
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
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
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
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
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
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
(2004) 64, 7110-7116
Reliable high-throughput functional screening with 3-FABS
Dalvit C, Ardini E, Fogliatto GP, Mongelli N, Veronesi M.
Drug Discovery Today
(2004) 9, 595-602
Kinase selectivity profiling by inhibitor affinity chromatography
Valsasina B, Kalisz H, Isacchi A
Expert Review Proteomics
(2004) 1 (3), 89-101
In vivo Assessment of Antiangiogenic Activity of SU6668 in an Experimental Colon Carcinoma Model
Marzola P, Degrassi A, Calderan L, Farace P, Crescimanno C, Nicolato E, Giusti A, Pesenti E, Terron A, Sbarbati A, Abrams T, Murray L, Osculati F
Clinical Cancer Research
(2004) 10, 739-750
Nicotinoyl Azide (NCA)-Mediated Mitsunoby Reaction: An Expedient One-Pot Transformation of Alcohols into Azides
Papeo G, Posteri H, Vianello P, Varasi M
Synthesis
(2004) 17, 2886-2892
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