Abstract
New indolylarylsulfone (IAS) derivatives bearing nitrogen containing substituents at the indole-2-carboxamide inhibited the HIV-1 WT in MT-4 cells at low nanomolar concentrations. In particular, compound 9 was uniformly effective against the mutant Y181C, Y188L, and K103N HIV-1 strains; it was highly active against the multidrug resistant mutant IRLL98 HIV-1 strain bearing the K101Q, Y181C, and G190A mutations conferring resistance to NVP, DLV, and EFV and several HIV-1 clades A in PBMC.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Cell Line
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HIV Reverse Transcriptase / antagonists & inhibitors*
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HIV-1 / drug effects
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HIV-1 / enzymology*
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HIV-1 / genetics
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Indoles / chemistry*
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Mutation
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Nitrogen / chemistry*
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Reverse Transcriptase Inhibitors / chemistry
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Reverse Transcriptase Inhibitors / pharmacology
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Structure-Activity Relationship
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Sulfones / chemistry*
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Sulfones / pharmacology*
Substances
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Indoles
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Reverse Transcriptase Inhibitors
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Sulfones
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reverse transcriptase, Human immunodeficiency virus 1
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HIV Reverse Transcriptase
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Nitrogen