Mononucleoside phosphotriester derivatives with S-acyl-2-thioethyl bioreversible phosphate-protecting groups: intracellular delivery of 3'-azido-2', 3'- …

I Lefebvre, C Perigaud, A Pompon…

Index: Lefebvre, Isabelle; Perigaud, Christian; Pompon, Alain; Aubertin, Anne-Marie; Girardet, Jean-Luc; et al. Journal of Medicinal Chemistry, 1995 , vol. 38, # 20 p. 3941 - 3950

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Citation Number: 216

Abstract

The synthesis, in vitro anti-HIV-1 activity, and decomposition pathways of several mononucleoside phosphotriester derivatives of 3'-azido-2', 3'-dideoxythymidine (AZT) incorporating a new kind of carboxylate esterase-labile transient phosphate-protecting group, namely, S-acyl-2-thioethyl, are reported. All the described compounds showed marked antiviral activity in thymidine kinase-deficient CEM cells in which AZT was virtually ...