G. Gosselin et al., NEW INSIGHTS REGARDING THE POTENTIAL OF THE PRONUCLEOTIDE APPROACH INANTIVIRAL CHEMOTHERAPY, Acta Biochimica Polonica, 43(1), 1996, pp. 195-208
The rationale for a pronucleotide approach based on the use of phospho
triesters which incorporate enzyme-mediated bio-labile protection is d
iscussed in detail. Among the studied bio-labile phosphate protecting
groups, the S-acyl-2-thioethyl (SATE) groups appeared the most promisi
ng as exemplified in cell culture systems in the case of the pronucleo
tides of 3'-azido-3'-deoxythymidine, 2'3'-didehydro-3'-deoxythymidine,
2'3'-dideoxyadenosine and acyclovir. In vivo implementations of such
bis(SATE) pronucleotides have been planned for future animal studies.