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Indolylarylsulfones bearing natural and unnatural amino acids. Discovery of potent inhibitors of HIV-1 non-nucleoside wild type and resistant mutant strains reverse transcriptase and coxsackie B4 virus.
Piscitelli F, Coluccia A, Brancale A, La Regina G, Sansone A, Giordano C, Balzarini J, Maga G, Zanoli S, Samuele A, Cirilli R, La Torre F, Lavecchia A, Novellino E, Silvestri R. Piscitelli F, et al. Among authors: samuele a. J Med Chem. 2009 Apr 9;52(7):1922-34. doi: 10.1021/jm801470b. J Med Chem. 2009. PMID: 19281225
Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity.
Regina GL, Coluccia A, Piscitelli F, Bergamini A, Sinistro A, Cavazza A, Maga G, Samuele A, Zanoli S, Novellino E, Artico M, Silvestri R. Regina GL, et al. Among authors: samuele a. J Med Chem. 2007 Oct 4;50(20):5034-8. doi: 10.1021/jm070488f. Epub 2007 Sep 6. J Med Chem. 2007. PMID: 17803291
Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants.
Radi M, Maga G, Alongi M, Angeli L, Samuele A, Zanoli S, Bellucci L, Tafi A, Casaluce G, Giorgi G, Armand-Ugon M, Gonzalez E, Esté JA, Baltzinger M, Bec G, Dumas P, Ennifar E, Botta M. Radi M, et al. Among authors: samuele a. J Med Chem. 2009 Feb 12;52(3):840-51. doi: 10.1021/jm801330n. J Med Chem. 2009. PMID: 19140683
Specific targeting of highly conserved residues in the HIV-1 reverse transcriptase primer grip region. 2. Stereoselective interaction to overcome the effects of drug resistant mutations.
Butini S, Brindisi M, Cosconati S, Marinelli L, Borrelli G, Coccone SS, Ramunno A, Campiani G, Novellino E, Zanoli S, Samuele A, Giorgi G, Bergamini A, Di Mattia M, Lalli S, Galletti B, Gemma S, Maga G. Butini S, et al. Among authors: samuele a. J Med Chem. 2009 Feb 26;52(4):1224-8. doi: 10.1021/jm801395v. J Med Chem. 2009. PMID: 19170521
Enantioselective binding of second generation pyrrolobenzoxazepinones to the catalytic ternary complex of HIV-1 RT wild-type and L100I and K103N drug resistant mutants.
Butini S, Gemma S, Brindisi M, Borrelli G, Fiorini I, Samuele A, Karytinos A, Facchini M, Lossani A, Zanoli S, Campiani G, Novellino E, Focher F, Maga G. Butini S, et al. Among authors: samuele a. Bioorg Med Chem Lett. 2011 Jul 1;21(13):3935-8. doi: 10.1016/j.bmcl.2011.05.020. Epub 2011 May 14. Bioorg Med Chem Lett. 2011. PMID: 21636271
New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors.
La Regina G, Coluccia A, Brancale A, Piscitelli F, Famiglini V, Cosconati S, Maga G, Samuele A, Gonzalez E, Clotet B, Schols D, Esté JA, Novellino E, Silvestri R. La Regina G, et al. Among authors: samuele a. J Med Chem. 2012 Jul 26;55(14):6634-8. doi: 10.1021/jm300477h. Epub 2012 Jul 6. J Med Chem. 2012. PMID: 22712652
Dihydro-alkylthio-benzyl-oxopyrimidines as inhibitors of reverse transcriptase: synthesis and rationalization of the biological data on both wild-type enzyme and relevant clinical mutants.
Mugnaini C, Alongi M, Togninelli A, Gevariya H, Brizzi A, Manetti F, Bernardini C, Angeli L, Tafi A, Bellucci L, Corelli F, Massa S, Maga G, Samuele A, Facchini M, Clotet-Codina I, Armand-Ugón M, Esté JA, Botta M. Mugnaini C, et al. Among authors: samuele a. J Med Chem. 2007 Dec 27;50(26):6580-95. doi: 10.1021/jm0708230. Epub 2007 Dec 6. J Med Chem. 2007. PMID: 18052319
38 results