Intracellular delivery of bioactive AZT nucleotides by aryl phosphate derivatives of AZT

C McGuigan, RN Pathirana, J Balzarini…

Index: McGuigan; Pathirana; Balzarini; De Clercq Journal of Medicinal Chemistry, 1993 , vol. 36, # 8 p. 1048 - 1052

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Citation Number: 230

Abstract

Novel aryl phosphate derivatives of the anti-HIV nucleoside analogue AZT have been prepared by phosphorochloridate chemistry. These materials were designed to act as membrane-soluble prodrugs of the bioactive free nucleotides. In vitro evaluation revealed the compounds to have a pronounced, selective anti-HIV activity in CEM cells; the magnitude of the biological effect varied considerably depending on the nature of the ...