Résumé
It was demonstrated that the use of neutral 2′,3′-dideoxyuridine phosphotriesters which incorporate enzyme mediated bioreversible protection such as S-acetylthioethanol (SATE) or dithiodiethanol (DTE) resulted in intracellular delivery of the parent mononucleotide. This point was corroborated by observation of an anti-HIV effect in various cell lines and decomposition data in cell extracts.
Cytosolic delivery of nucleoside monophosphate has been achieved by the use of neutral 2′,3′-dideoxyuridine phosphotriesters incorporating enzymatically bioreversible protection with S-acetylthioethanol (SATE) or dithiodiethanol (DTE).