Abstract
Synthesis of phosphorylated derivatives of ribavirin was accomplished in two steps. In the first step, 4-chlorophenyl dichlorophosphate was reacted with various amines and alcohols in equimolar quantities in the presence of triethylamine. These intermediate monochlorides were further treated with ribavirine (RBV) using Et3N as a base at 0-30 ºC in pyridine and THF. All the title compounds were purified by column chromatography and characterized by spectral data. Based on the importance of nucleoside in anticancer activity, their cytotoxicity was evaluated against lung cancer cell lines (NCI-69). Majority of the title compounds exhibited high activity. These results will be supported further for development of phosphorylated nucleosides.
