Abstract
Indolyl aryl sulfones bearing the 4,5-difluoro (10) or 5-chloro-4-fluoro (16) substitution pattern at the indole ring were potent inhibitors of HIV-1 WT and the NNRTI-resistant strains Y181C and K103N-Y181C. These compounds were highly effective against the 112 and the AB1 strains in lymphocytes and inhibited at nanomolar concentration the multiplication of the IIIBBa-L strain in macrophages. Compound 16 was exceptionally potent against RT WT and RTs carrying the K103N, Y181I, and L100I mutations.
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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Drug Resistance, Viral
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HIV Reverse Transcriptase / genetics
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HIV Reverse Transcriptase / metabolism*
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HIV-1 / drug effects*
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HIV-1 / enzymology
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Humans
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In Vitro Techniques
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Indoles / chemical synthesis*
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Indoles / chemistry
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Indoles / pharmacology
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Lymphocytes / drug effects
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Lymphocytes / virology
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Macrophages / drug effects
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Macrophages / virology
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Reverse Transcriptase Inhibitors / chemical synthesis*
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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 / chemical synthesis*
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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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HIV Reverse Transcriptase