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Discovery of (7R)-14-cyclohexyl-7-{[2-(dimethylamino)ethyl](methyl) amino}-7,8-dihydro-6H-indolo[1,2-e][1,5]benzoxazocine-11-carboxylic acid (MK-3281), a potent and orally bioavailable finger-loop inhibitor of the hepatitis C virus NS5B polymerase.
Narjes F, Crescenzi B, Ferrara M, Habermann J, Colarusso S, Ferreira Mdel R, Stansfield I, Mackay AC, Conte I, Ercolani C, Zaramella S, Palumbi MC, Meuleman P, Leroux-Roels G, Giuliano C, Fiore F, Di Marco S, Baiocco P, Koch U, Migliaccio G, Altamura S, Laufer R, De Francesco R, Rowley M. Narjes F, et al. Among authors: palumbi mc. J Med Chem. 2011 Jan 13;54(1):289-301. doi: 10.1021/jm1013105. Epub 2010 Dec 8. J Med Chem. 2011. PMID: 21141896
Inhibitors of the hepatitis C virus NS3 protease with basic amine functionality at the P3-amino acid N-terminus: discovery and optimization of a new series of P2-P4 macrocycles.
Harper S, Ferrara M, Crescenzi B, Pompei M, Palumbi MC, DiMuzio JM, Donghi M, Fiore F, Koch U, Liverton NJ, Pesci S, Petrocchi A, Rowley M, Summa V, Gardelli C. Harper S, et al. Among authors: palumbi mc. J Med Chem. 2009 Aug 13;52(15):4820-37. doi: 10.1021/jm900372w. J Med Chem. 2009. PMID: 19624135
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.
Jones P, Altamura S, Boueres J, Ferrigno F, Fonsi M, Giomini C, Lamartina S, Monteagudo E, Ontoria JM, Orsale MV, Palumbi MC, Pesci S, Roscilli G, Scarpelli R, Schultz-Fademrecht C, Toniatti C, Rowley M. Jones P, et al. Among authors: palumbi mc. J Med Chem. 2009 Nov 26;52(22):7170-85. doi: 10.1021/jm901188v. J Med Chem. 2009. PMID: 19873981
Identification of novel, selective, and stable inhibitors of class II histone deacetylases. Validation studies of the inhibition of the enzymatic activity of HDAC4 by small molecules as a novel approach for cancer therapy.
Ontoria JM, Altamura S, Di Marco A, Ferrigno F, Laufer R, Muraglia E, Palumbi MC, Rowley M, Scarpelli R, Schultz-Fademrecht C, Serafini S, Steinkühler C, Jones P. Ontoria JM, et al. Among authors: palumbi mc. J Med Chem. 2009 Nov 12;52(21):6782-9. doi: 10.1021/jm900555u. J Med Chem. 2009. PMID: 19888759
Identification of MK-5710 ((8aS)-8a-methyl-1,3-dioxo-2-[(1S,2R)-2-phenylcyclo- propyl]-N-(1-phenyl-1H-pyrazol-5-yl)hexahydro-imidazo[1,5-a]pyrazine-7(1H)-carboxamide), a potent smoothened antagonist for use in Hedgehog pathway dependent malignancies, part 2.
Kinzel O, Alfieri A, Altamura S, Brunetti M, Bufali S, Colaceci F, Ferrigno F, Filocamo G, Fonsi M, Gallinari P, Malancona S, Hernando JI, Monteagudo E, Orsale MV, Palumbi MC, Pucci V, Rowley M, Sasso R, Scarpelli R, Steinkühler C, Jones P. Kinzel O, et al. Among authors: palumbi mc. Bioorg Med Chem Lett. 2011 Aug 1;21(15):4429-35. doi: 10.1016/j.bmcl.2011.06.023. Epub 2011 Jun 16. Bioorg Med Chem Lett. 2011. PMID: 21737263
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