Regioselective synthesis and anticancer evaluation of H2O2-activable nucleosides.

We describe here the design, synthesis, and biological evaluation of H2O2-activatable nucleosides via an efficient and regioselective functionalization of unprotected precursors. Biological evaluation of a H2O2-specific responsive prodrug of gemecitabin demonstrates an extremely fast activation, low toxicity and enhanced anticancer effects in two cell lines.