Synthesis and biological evaluation of 1,2,5-oxadiazole N-oxide derivatives as potential hypoxic cytotoxins and DNA-binders

Several new 1,2,5-oxadiazole N-oxide derivatives were syntheized to be test ed both as potential selective hypoxic cell cytotoxins and as DNA-binding a gents. The compounds prepared included his(1,2,5-oxadiazole N-oxide) deriva tives and oxadiazole rings linked to naphthyl residues. The compounds were tested for their cytotoxicity in oxia and hypoxia and they proved to be non -selective and less active than the parent compounds 3-formyl-4-phenyl-1,2, 5-oxadiazole N-2-oxide (3) and 3-chloromethyl-4-phenyl-1,2,5-oxadiazole N-2 -oxide (4). The DNA-affinity assays showed that the compounds tested have p oor affinity for this biomolecule.