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High potency of indolyl aryl sulfone nonnucleoside inhibitors towards drug-resistant human immunodeficiency virus type 1 reverse transcriptase mutants is due to selective targeting of different mechanistic forms of the enzyme.
Cancio R, Silvestri R, Ragno R, Artico M, De Martino G, La Regina G, Crespan E, Zanoli S, Hübscher U, Spadari S, Maga G. Cancio R, et al. Among authors: zanoli s. Antimicrob Agents Chemother. 2005 Nov;49(11):4546-54. doi: 10.1128/AAC.49.11.4546-4554.2005. Antimicrob Agents Chemother. 2005. PMID: 16251294 Free PMC article.
Selective targeting of the HIV-1 reverse transcriptase catalytic complex through interaction with the "primer grip" region by pyrrolobenzoxazepinone non-nucleoside inhibitors correlates with increased activity towards drug-resistant mutants.
Zanoli S, Gemma S, Butini S, Brindisi M, Joshi BP, Campiani G, Fattorusso C, Persico M, Crespan E, Cancio R, Spadari S, Hübscher U, Maga G. Zanoli S, et al. Biochem Pharmacol. 2008 Jul 15;76(2):156-68. doi: 10.1016/j.bcp.2008.04.009. Epub 2008 Apr 29. Biochem Pharmacol. 2008. PMID: 18541223
Toward the discovery of novel anti-HIV drugs. Second-generation inhibitors of the cellular ATPase DDX3 with improved anti-HIV activity: synthesis, structure-activity relationship analysis, cytotoxicity studies, and target validation.
Maga G, Falchi F, Radi M, Botta L, Casaluce G, Bernardini M, Irannejad H, Manetti F, Garbelli A, Samuele A, Zanoli S, Esté JA, Gonzalez E, Zucca E, Paolucci S, Baldanti F, De Rijck J, Debyser Z, Botta M. Maga G, et al. Among authors: zanoli s. ChemMedChem. 2011 Aug 1;6(8):1371-89. doi: 10.1002/cmdc.201100166. Epub 2011 Jun 22. ChemMedChem. 2011. PMID: 21698775
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: zanoli s. J Med Chem. 2007 Oct 4;50(20):5034-8. doi: 10.1021/jm070488f. Epub 2007 Sep 6. J Med Chem. 2007. PMID: 17803291
48 results