Aryl phosphate derivates of AZT inhibit HIV replication in cells where the nucleoside is poorly active

Bioorganic & Medicinal Chemistry Letters
1992.0

Abstract

Phosphate derivatives of the anti-HIV nucleoside analogue AZT were prepared as potential pro-drugs of the bio-active free nucleotide. In marked contrast to the parent nucleoside AZT, several of the derivatives are active inhibitors of HIV in kinase-deficient cells. The precise activity varies greatly with the phosphate structure, data consistent with a mode of action involving intracellular hydrolysis to release the bio-active nucleotide forms.

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