Abstract
The potency and selectivity index of the AZT-phenyl phosphate derivatives in thymidine kinase (TK)-deficient T cells were substantially enhanced by introducing a single para-bromo substitutent in the phenyl moiety. AZT-5'-(p-bromophenyl methoxyalaninyl phosphate) was 43-fold more potent than AZT-5'-(phenyl methoxyalaninyl phosphate) and was fivefold more potent than AZT in inhibiting human immunodeficiency virus (HIV) replication in TK-deficient CEM cells.
MeSH terms
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Anti-HIV Agents / chemical synthesis
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Anti-HIV Agents / pharmacology*
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Dideoxynucleotides
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HIV Reverse Transcriptase / antagonists & inhibitors
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HIV-1 / drug effects
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HIV-1 / enzymology
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HIV-1 / genetics
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Humans
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Organophosphorus Compounds / pharmacology
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Organophosphorus Compounds / therapeutic use*
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Thymine Nucleotides
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Virus Replication / drug effects
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Virus Replication / genetics
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Zidovudine / analogs & derivatives*
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Zidovudine / chemical synthesis
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Zidovudine / pharmacology*
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Zidovudine / therapeutic use
Substances
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3'-azido-3'-deoxythymidine-5'-(4-bromophenyl methoxyalaninyl phosphate)
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Anti-HIV Agents
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Dideoxynucleotides
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Organophosphorus Compounds
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Thymine Nucleotides
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Zidovudine
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HIV Reverse Transcriptase