Synthesis of a Heterocyclic Aza-Enediyne and Its DNA-Cleavage Properties.

Abstract The benzimidazolium salt 2 , incorporating an aza-enediyne moiety, has been prepared and is shown to be a very effective DNA-cleavage agent under mild physiological conditions. Its mechanism of action is currently under investigation but may involve the generation of a diradical intermediate, DNA alkylation, or both.