Design of new mononucleotide prodrugs: aryl (SATE) phosphotriester derivatives |
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| Authors: | Peyrottes S Schlienger N Beltran T Lefebvre I Pompon A Gosselin G Aubertin A M Imbach J L Périgaud C |
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| Institution: | UMR 5625 CNRS-UM II, Université Montpellier II, cc 008, place E. Bataillon, 34095 Montpellier, France. |
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| 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. |
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