Abstract
Human immunodeficiency virus type 1 (HIV-1) Rev protein facilitates the export of viral RNA from nucleus to cytoplasm, which is a key step in HIV-1 pathogenesis and transmission. In this study, we have screened a commercial library and identified the hit compound 1 bearing a benzenesulfonamide quinoline scaffold that inhibited Rev activity and HIV-1 infectivity. Compounds bearing this scaffold were synthesized and their SAR was studied. We identified compound 20 with low toxicity and potent activity to inhibit HIV-1 replication by affecting Rev function.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Anti-HIV Agents / chemical synthesis
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Anti-HIV Agents / chemistry
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Anti-HIV Agents / pharmacology*
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Benzene Derivatives / chemical synthesis
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Benzene Derivatives / chemistry
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Benzene Derivatives / pharmacology*
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Gene Products, rev / antagonists & inhibitors*
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Gene Products, rev / metabolism
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HIV-1 / drug effects*
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HIV-1 / growth & development
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HIV-1 / metabolism
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Molecular Structure
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Quinolines / chemical synthesis
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Quinolines / chemistry
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Quinolines / pharmacology*
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Sulfonamides / chemical synthesis
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Sulfonamides / chemistry
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Sulfonamides / pharmacology*
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Virus Replication / drug effects*
Substances
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Anti-HIV Agents
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Benzene Derivatives
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Gene Products, rev
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Quinolines
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Sulfonamides