Synthesis and biological activity of a gemcitabine phosphoramidate prodrug.
Basic Information
ID: ALA1146216
Journal: J Med Chem
Title: Synthesis and biological activity of a gemcitabine phosphoramidate prodrug.
Authors: Wu W, Sigmond J, Peters GJ, Borch RF.
Abstract: A gemcitabine (2',2'-difluorodeoxycytidine, dFdC) phosphoramidate prodrug designed for the intracellular delivery of gemcitabine 5'-monophosphate was synthesized. The prodrug was about an order of magnitude less active than gemcitabine against wild-type cells, and the nucleoside transport inhibitor dipyridamole reduced prodrug activity. The prodrug was more active than gemcitabine against two deoxycytidine kinase-deficient cell lines. The results suggest that the prodrug is a potent growth inhibitor that can bypass dCK deficiency at higher drug concentrations.
CiteXplore: 17602464
DOI: 10.1021/jm070269u
Patent ID: ┄