Abstract
Compounds having methyl, vinyl, and ethynyl groups at the 4'-position of stavudine (d4T: 2',3'-didehydro-3'-deoxythymidine) were synthesized. The compounds were assayed for their ability to inhibit the replication of HIV in cell culture. The 4'-ethynyl analogue (15) was found to be more potent and less toxic than the parent compound stavudine.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Anti-HIV Agents / chemical synthesis*
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Anti-HIV Agents / pharmacology*
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Cells, Cultured
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Humans
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Magnetic Resonance Spectroscopy
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Molecular Conformation
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Stavudine / analogs & derivatives*
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Stavudine / chemical synthesis
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Stavudine / chemistry*
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Stavudine / pharmacology*
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Structure-Activity Relationship
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Virus Replication / drug effects
Substances
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Anti-HIV Agents
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2',3'-didehydro-3'-deoxy-4'-ethynylthymidine
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Stavudine