A Series of Enediynes as Novel Inhibitors of Topoisomerase I Original Research Article

A series of acyclic enediynes, 2-((6-substituted)-3-hexen-1,5-diynyl)benzonitriles (8–11), display potent inhibition against topoisomerase I without the formation of active biradical intermediates and show inhibitory activity against topoisomerase I at 10 μM, which is five times that of camptothecin from the results of agarose gel electrophoresis.