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Article

New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.

European journal of medicinal chemistry - 15 Dec 2020

Nalli Marianna, Armijos Rivera Jorge I, Masci Domiziana, Coluccia Antonio, Badia Roger, Riveira-Muñoz Eva, Brambilla Alessandro, Cinquina Elisabetta, Turriziani Ombretta, Falasca Francesca, Catalano Myriam, Limatola Cristina, Esté José A, Maga Giovanni, Silvestri Romano, Crespan Emmanuele, La Regina Giuseppe

Abstract excerpt

We designed and synthesized 21 new indolylarylsulfones (IASs) as new HIV-1 NNRTIs. Among these, IAS 12 exhibited a remarkable antiviral activity against single and double mutants (K103N EC50 = <0.7 nM; Y181C EC50 = <0.7 nM; Y188L EC50 = 21.3 nM; K103N-Y181C EC50 = 6.2 nM), resulting equally or more active than previuosly reported IAS 6 and some approved anti-HIV-1 drugs. Docking and molecular dynamics simulations...

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Identifiers

PMID: 32883642
DOI: 10.1016/j.ejmech.2020.112696

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 6 Sept 2026. Manifest publication-graph-cohort-2026-09-06.1.

Source receipt: pubmed, retrieved 6 Sept 2026.

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