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Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection.
Summa V, Petrocchi A, Bonelli F, Crescenzi B, Donghi M, Ferrara M, Fiore F, Gardelli C, Gonzalez Paz O, Hazuda DJ, Jones P, Kinzel O, Laufer R, Monteagudo E, Muraglia E, Nizi E, Orvieto F, Pace P, Pescatore G, Scarpelli R, Stillmock K, Witmer MV, Rowley M. Summa V, et al. J Med Chem. 2008 Sep 25;51(18):5843-55. doi: 10.1021/jm800245z. J Med Chem. 2008. PMID: 18763751
Development of substituted 6-[4-fluoro-3-(piperazin-1-ylcarbonyl)benzyl]-4,5-dimethylpyridazin-3(2H)-ones as potent poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors active in BRCA deficient cells.
Ferrigno F, Branca D, Kinzel O, Lillini S, Llauger Bufi L, Monteagudo E, Muraglia E, Rowley M, Schultz-Fademrecht C, Toniatti C, Torrisi C, Jones P. Ferrigno F, et al. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1100-5. doi: 10.1016/j.bmcl.2009.11.087. Epub 2009 Nov 22. Bioorg Med Chem Lett. 2010. PMID: 20022747
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. 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
34 results