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).