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Page 1
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 N, Ballinari D, Cameron A, Casale E, Cervi G, Colombo M, Colotta F, Croci V, D'Alessio R, Fiorentini F, Isacchi A, Mercurio C, Moretti W, Panzeri A, Pastori W, Pevarello P, Quartieri F, Roletto F, Traquandi G, Vianello P, Vulpetti A, Ciomei M. Brasca MG, et al. Among authors: casale e. J Med Chem. 2009 Aug 27;52(16):5152-63. doi: 10.1021/jm9006559. J Med Chem. 2009. PMID: 19603809
3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 1. Lead finding.
Pevarello P, Brasca MG, Amici R, Orsini P, Traquandi G, Corti L, Piutti C, Sansonna P, Villa M, Pierce BS, Pulici M, Giordano P, Martina K, Fritzen EL, Nugent RA, Casale E, Cameron A, Ciomei M, Roletto F, Isacchi A, Fogliatto G, Pesenti E, Pastori W, Marsiglio A, Leach KL, Clare PM, Fiorentini F, Varasi M, Vulpetti A, Warpehoski MA. Pevarello P, et al. Among authors: casale e. J Med Chem. 2004 Jun 17;47(13):3367-80. doi: 10.1021/jm031145u. J Med Chem. 2004. PMID: 15189033
Optimization 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. Brasca MG, et al. Among authors: casale e. Bioorg Med Chem. 2010 Mar 1;18(5):1844-53. doi: 10.1016/j.bmc.2010.01.042. Epub 2010 Jan 25. Bioorg Med Chem. 2010. PMID: 20153204
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. Brasca MG, et al. Among authors: casale e. Bioorg Med Chem. 2013 Nov 15;21(22):7047-63. doi: 10.1016/j.bmc.2013.09.018. Epub 2013 Sep 19. Bioorg Med Chem. 2013. PMID: 24100158
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. Papeo G, et al. Among authors: casale e. J Med Chem. 2015 Sep 10;58(17):6875-98. doi: 10.1021/acs.jmedchem.5b00680. Epub 2015 Aug 26. J Med Chem. 2015. PMID: 26222319
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. Polucci P, et al. Among authors: casale e. J Med Chem. 2013 Jan 24;56(2):437-50. doi: 10.1021/jm3013213. Epub 2013 Jan 4. J Med Chem. 2013. PMID: 23245311
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 E, Pesenti E, Galvani A, Mantegani S, Isacchi A. Fogliatto G, et al. Among authors: casale e. Clin Cancer Res. 2013 Jul 1;19(13):3520-32. doi: 10.1158/1078-0432.CCR-12-3512. Epub 2013 May 14. Clin Cancer Res. 2013. PMID: 23674492
74 results