Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors.

doi:10.1021/jm901188v

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Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors.

Journal of medicinal chemistry - 26 Nov 2009

Jones Philip, Altamura Sergio, Boueres Julia, Ferrigno Federica, Fonsi Massimiliano, Giomini Claudia, Lamartina Stefania, Monteagudo Edith, Ontoria Jesus M, Orsale Maria Vittoria, Palumbi Maria Cecilia, Pesci Silvia, Roscilli Giuseppe, Scarpelli Rita, Schultz-Fademrecht Carsten, Toniatti Carlo, Rowley Michael

Abstract excerpt

We disclose the development of a novel series of 2-phenyl-2H-indazole-7-carboxamides as poly(ADP-ribose)polymerase (PARP) 1 and 2 inhibitors. This series was optimized to improve enzyme and cellular activity, and the resulting PARP inhibitors display antiproliferation activities against BRCA-1 and BRCA-2 deficient cancer cells, with high selectivity over BRCA proficient cells. Extrahepatic oxidation by CYP450 1A1...

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PMID: 19873981
DOI: 10.1021/jm901188v

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