Naphthyl phosphoramidate derivatives of BVdU as potential anticancer agents: Design, synthesis and biological evaluation

The phosphoramidate technology we have developed has been recently applied to BVdU, leading to NB1011 (NewBiolics Inc., California), a novel potential anticancer compound recently entered into Phase 2 of the clinical trials for colon cancer. We report in this work a new series of derivatives containing naphthol as aryl masking group on the phosphate moiety, which has shown a significant increase in anticancer activity in preliminary biological evaluations.