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

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 =

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Bibliographic Details
Published in:European journal of medicinal chemistry 2020-12, Vol.208, p.112696-112696, Article 112696
Main Authors: 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
Format: Article
Language:English
Subjects:
AIDS
HIV-1
Indolylarylsulfone
Non-nucleoside reverse transcriptase inhibitor
Reverse transcriptase
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Summary: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 =
ISSN:0223-5234
1768-3254
DOI:10.1016/j.ejmech.2020.112696