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Original Articles

DESIGN OF NEW MONONUCLEOTIDE PRODRUGS: ARYL (SATE) PHOSPHOTRIESTER DERIVATIVES

, , , , , , , & show all
Pages 315-321 | Published online: 07 Feb 2007
 

Abstract

Synthesis, biological activities and decomposition kinetics of novel phosphotriester derivatives of 3′-azido-2′,3′-dideoxythymidine (AZT) bearing a S-tButyl-2-thioethyl (tBuSATE) group and L-tyrosinyl residues are reported. All the derivatives appeared to be potent inhibitors of HIV-1 replication in various cell culture experiments. The proposed decomposition process of these mixed phosphotriesters may involve successively an esterase and then a phosphodiesterase activation.

ACKNOWLEDGMENTS

These investigations were supported by grants from the Agence Nationale de Recherches sur le SIDA (ANRS) and the Fondation pour la Recherche Médicale (FRM).

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