Abstract
Two thia-DCK analogs (3a,b) were synthesized and evaluated for inhibition of HIV-1 replication in H9 lymphocytes. Compound 3a showed potent anti-HIV activity with an EC50 value of 0.14 microM and a therapeutic index of 1110. However, the corresponding 6-tert-butyl-substituted compound (3b) showed no suppression. The bioassay results indicated that thia-DCK analogs merit attention as potential HIV-1 inhibitors.
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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Cell Line
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HIV / drug effects
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Humans
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Inhibitory Concentration 50
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Lactones / chemical synthesis
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Lactones / pharmacology
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Lymphocytes / virology
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Structure-Activity Relationship
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Thiones / chemical synthesis
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Thiones / pharmacology
Substances
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Anti-HIV Agents
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Lactones
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Thiones