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Page 1
Optimization of a series of potent and selective ketone histone deacetylase inhibitors.
Pescatore G, Kinzel O, Attenni B, Cecchetti O, Fiore F, Fonsi M, Rowley M, Schultz-Fademrecht C, Serafini S, Steinkühler C, Jones P. Pescatore G, et al. Among authors: jones p. Bioorg Med Chem Lett. 2008 Oct 15;18(20):5528-32. doi: 10.1016/j.bmcl.2008.09.003. Epub 2008 Sep 6. Bioorg Med Chem Lett. 2008. PMID: 18809328
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. J Med Chem. 2009 Nov 26;52(22):7170-85. doi: 10.1021/jm901188v. J Med Chem. 2009. PMID: 19873981
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: jones p. 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
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. Among authors: jones p. J Med Chem. 2008 Sep 25;51(18):5843-55. doi: 10.1021/jm800245z. J Med Chem. 2008. PMID: 18763751
Studies of the metabolic stability in cells of 5-(trifluoroacetyl)thiophene-2-carboxamides and identification of more stable class II histone deacetylase (HDAC) inhibitors.
Scarpelli R, Di Marco A, Ferrigno F, Laufer R, Marcucci I, Muraglia E, Ontoria JM, Rowley M, Serafini S, Steinkühler C, Jones P. Scarpelli R, et al. Among authors: jones p. Bioorg Med Chem Lett. 2008 Dec 1;18(23):6078-82. doi: 10.1016/j.bmcl.2008.10.041. Epub 2008 Oct 12. Bioorg Med Chem Lett. 2008. PMID: 18952417
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: jones p. J Med Chem. 2009 Nov 12;52(21):6782-9. doi: 10.1021/jm900555u. J Med Chem. 2009. PMID: 19888759
8,809 results