Design and synthesis of heterocycle fused enediyne prodrugs activable at will

Abstract

In this account we report our efforts to prepare simplified analogues of natural occurring enediynes during the last ten years. We have succeeded in preparing two different classes of such compounds were the embedded 10-membered enediyne system is fused either with a β-lactam ring or with an epoxide. Biological tests on these compounds have demonstrated that some representatives are able to cleave the double strand of DNA even at very low concentrations; efforts have also been devoted to make these compounds active only under controlled conditions. ©ARKAT.