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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, 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: 28 Jun 2019 02:29

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