Abstract
CycloSal-d4TMP and two different bis(benzyl) phosphate triesters of the antivirally active nucleoside analog d4T were studied with regard to their chemical hydrolysis behavior at pH 7.3, in CEM/0 cell extracts, and their anti-HIV activity. In contrast to triesters 2-4, bis-(o-AB)-d4TMP 1 was found to be chemically exquisitely stable. All compounds led to the formation of d4TMP in cell extracts and all triesters achieved the TK-bypass.
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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Antiviral Agents / chemical synthesis*
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Antiviral Agents / chemistry
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Antiviral Agents / pharmacology
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Benzyl Compounds
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Dideoxynucleotides
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Drug Design
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Drug Stability
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Humans
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Hydrolysis
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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 / pharmacokinetics
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Tumor Cells, Cultured
Substances
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2',3'-dideoxy-2',3'-didehydrothymidine monophosphate
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Anti-HIV Agents
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Antiviral Agents
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Benzyl Compounds
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Dideoxynucleotides
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Stavudine