Novel N-oxide of naphthalimides as prodrug leads against hypoxic solid tumor: Synthesis and biological evaluation

Novel tertiary amine N-oxides of naphthalimides were designed and synthesized as potential anticancer agents against hypoxic solid tumors. Although their ctDNA-binding affinities and cytotoxic activities against usual tumor cell lines were lower than those of corresponding amines, the N-oxides A1 and A4 showed hypoxia preference activities against A375 cells in vitro and might be used as interesting candidates of prodrug leads in hypoxic tumor cells.