Abstract
Phosphoramidate pronucleotides have proven to be an effective strategy for the intracellular delivery of nucleoside 5-monophosphates. This review will summarize our efforts to understand the in vitro and in vivo behavior of phosphoramidate monoesters of 3-azido-3-deoxythymidine (AZT), 3-fluoro-3- deoxythymidine (FLT) and 5-fluoro-2-deoxyuridine (FUdR). Insights drawn from these studies have proved valuable for the future design of phosphoramidate-based pronucleotides.
Keywords: pronucleotide stratagem, phosphoramidates, antiviral pyrimidines, nucleoside monophosphates