2012
- 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
Italo Beria, Michele Caruso, Barbara Valsasina, Dario, Ballinari, Jay Bertrand, Maria Gabriella Brasca, Marina Caldarelli, Paolo Cappella, Francesco Fiorentini, Laura M. Gianellini, Alessandra Scolaro.
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
- 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. - 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
(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