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New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors

Famiglini, Valeria, La Regina, Giuseppe, Coluccia, Antonio, Pelliccia, Sveva, Brancale, Andrea ORCID:, Maga, Giovanni, Crespan, Emmanuele, Badia, Roger, Clotet, Bonaventura, Esté, José A., Cirilli, Roberto, Novellino, Ettore and Silvestri, Romano 2014. New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. European Journal of Medicinal Chemistry 80 , pp. 101-111. 10.1016/j.ejmech.2014.04.027

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New indolylarylsulfone HIV-1 NNRTIs were synthesized to evaluate unexplored substitutions of the benzyl/phenylethyl group linked at the indole-2-carboxamide. Against the NL4-3 HIV-1 WT strain, 17 out 20 compounds were superior to NVP and EFV. Several compounds inhibited the K103N HIV-1 mutant strain at nanomolar concentration and were superior to EFV. Some derivatives were superior to EFV against the Y181C and L100I HIV-1 mutant strains. Against the NL4-3 HIV-1 strain, the enantiomers 24 and 25 showed small differences of activity. In contrast, 24 turned out significantly more potent than 25 against the whole panel of mutant HIV-1 strains. The docking studies suggested that the difference in the observed inhibitory activities of 24 and 25 against the K03N mutation could be due to a kinetic rather than affinity differences.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Pharmacy
Subjects: Q Science > QR Microbiology > QR180 Immunology
Q Science > QR Microbiology > QR355 Virology
R Medicine > RM Therapeutics. Pharmacology
Uncontrolled Keywords: AIDS; HIV-1; Reverse transcriptase; Nonnucleoside inhibitor; Indolylarylsulfone
Publisher: Elsevier
ISSN: 0223-5234
Date of First Compliant Deposit: 30 March 2016
Date of Acceptance: 7 April 2014
Last Modified: 10 Nov 2023 08:17

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