A novel benzimidazole-imidazo[1,2-a]pyridine hybrid; 2-(imidazo[1,2-a]pyridine-8-yl)benzimidazole and its symmetrical bis- derivative 2,2 '-bis-(imidazo[1,2-a]pyridine-8-yl)-1H,1H '-[5,5 ']-bisbenzimidazole were synthesized and characterized. It was found that these two compounds have a strong DNA groove binding and peroxide mediated DNA-cleavage properties. Furthermore, these molecules were screened against three different human cell lines namely HepG2, DLD-1 and MDA-MB-231, and these compounds were found to have high cytotoxic activities.