A series of acyclic enediynes, 2-((6-substituted)-3-hexen- 1,5-diynyl)benzo
nitriles (8-11), display potent inhibition against topoisomerase I without
the formation of active biradical intermediates and show inhibitory activit
y against topoisomerase I at 10 muM, which is five times that of camptothec
in from the results of agarose gel electrophoresis. (C) 2001 Elsevier Scien
ce Ltd. All rights reserved.