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Page 1
Discovery and synthesis of HIV integrase inhibitors: development of potent and orally bioavailable N-methyl pyrimidones.
Gardelli C, Nizi E, Muraglia E, Crescenzi B, Ferrara M, Orvieto F, Pace P, Pescatore G, Poma M, Ferreira Mdel R, Scarpelli R, Homnick CF, Ikemoto N, Alfieri A, Verdirame M, Bonelli F, Paz OG, Taliani M, Monteagudo E, Pesci S, Laufer R, Felock P, Stillmock KA, Hazuda D, Rowley M, Summa V. Gardelli C, et al. Among authors: laufer r. J Med Chem. 2007 Oct 4;50(20):4953-75. doi: 10.1021/jm0704705. Epub 2007 Sep 8. J Med Chem. 2007. PMID: 17824681
Dihydroxypyrimidine-4-carboxamides as novel potent and selective HIV integrase inhibitors.
Pace P, Di Francesco ME, Gardelli C, Harper S, Muraglia E, Nizi E, Orvieto F, Petrocchi A, Poma M, Rowley M, Scarpelli R, Laufer R, Gonzalez Paz O, Monteagudo E, Bonelli F, Hazuda D, Stillmock KA, Summa V. Pace P, et al. Among authors: laufer r. J Med Chem. 2007 May 3;50(9):2225-39. doi: 10.1021/jm070027u. Epub 2007 Apr 12. J Med Chem. 2007. PMID: 17428043
Design and synthesis of bicyclic pyrimidinones as potent and orally bioavailable HIV-1 integrase inhibitors.
Muraglia E, Kinzel O, Gardelli C, Crescenzi B, Donghi M, Ferrara M, Nizi E, Orvieto F, Pescatore G, Laufer R, Gonzalez-Paz O, Di Marco A, Fiore F, Monteagudo E, Fonsi M, Felock PJ, Rowley M, Summa V. Muraglia E, et al. Among authors: laufer r. J Med Chem. 2008 Feb 28;51(4):861-74. doi: 10.1021/jm701164t. Epub 2008 Jan 25. J Med Chem. 2008. PMID: 18217703
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: laufer r. 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: laufer r. 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: laufer r. J Med Chem. 2009 Nov 12;52(21):6782-9. doi: 10.1021/jm900555u. J Med Chem. 2009. PMID: 19888759
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: laufer r. J Med Chem. 2011 Jan 13;54(1):289-301. doi: 10.1021/jm1013105. Epub 2010 Dec 8. J Med Chem. 2011. PMID: 21141896
141 results