Abstract
Synthesis and biological activities of several phosphotriester derivatives of 3'-azido-2',3'-dideoxythymidine (AZT) bearing a S-pivaloyl-2-thioethyl (tBuSATE) group and aryl residues derived from L-tyrosine are reported. All compounds showed marked anti-HIV activity in thymidine kinase-deficient CEM cells demonstrating their ability to deliver intracellularly the parent 5'-mononucleotide.
MeSH terms
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Anti-HIV Agents / chemical synthesis*
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Anti-HIV Agents / pharmacokinetics
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Anti-HIV Agents / pharmacology
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Biological Transport
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Cell Line
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Dideoxynucleotides
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HIV / drug effects*
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Humans
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Molecular Structure
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Thymidine Kinase / deficiency
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Thymine Nucleotides / pharmacokinetics
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Zidovudine / analogs & derivatives*
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Zidovudine / chemical synthesis
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Zidovudine / pharmacokinetics
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Zidovudine / pharmacology
Substances
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Anti-HIV Agents
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Dideoxynucleotides
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Thymine Nucleotides
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Zidovudine
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zidovudine triphosphate
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Thymidine Kinase