A series of enediynes as novel inhibitors of topoisomerase I

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 muM, which is five times that of camptothecin from the results of agarose gel electrophoresis. (C) 2001 Elsevier Science Ltd. All rights reserved.