Discovery, characterization, and lead optimization of 7-azaindole non-nucleoside HIV-1 reverse transcriptase inhibitors

A library of 585 compounds built off a 7-azaindole core was evaluated for anti-HIV-1 activity, and ten hits emerged with submicromolar potency and therapeutic index >100. Of these, three were identified as non-nucleoside reverse transcriptase (RT) inhibitors and were assayed against relevant resi...

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Bibliographic Details
Published in:Bioorg Med Chem Lett
Main Authors: Stanton, Richard A., Lu, Xiao, Detorio, Mervi, Montero, Catherine, Hammond, Emily T., Ehteshami, Maryam, Domaoal, Robert A., Nettles, James H., Feraud, Michel, Schinazi, Raymond F.
Format: Artigo
Language:Inglês
Published: 2016
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Article
Online Access:https://ncbi.nlm.nih.gov/pmc/articles/PMC7720368/
https://ncbi.nlm.nih.gov/pubmed/27390064
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2016.06.065
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