M. Lorey et al., LO-SALIGENYL-5-FLUORO-2'-DEOXYURIDINEMONOPHOSPHATE (CYCLOSAL-FDUMP) -A NEW PRODRUG APPROACH FOR FDUMP, Nucleosides & nucleotides, 16(7-9), 1997, pp. 1307-1310
The synthesis of cycloSal-FdUMP 3a-d as a new prodrug approach for FdU
1 is described. Phosphotriesters 3 release the FdUMP 2 selectively by
a controlled, chemically induced tandem reaction in hydrolysis studie
s. The biological activity (IC50) of cycloSal-phosphotriesters 3 was e
valuated in FM3A/O cells and FM3A/TK- cells.