A series of enediynes as novel inhibitors of topoisomerase I

Bioorg Med Chem. 2001 Jul;9(7):1707-11. doi: 10.1016/s0968-0896(01)00081-5.

Abstract

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 microM, which is five times that of camptothecin from the results of agarose gel electrophoresis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Camptothecin / pharmacology
  • Electrophoresis, Agar Gel
  • Enzyme Inhibitors / pharmacology*
  • Nitriles / pharmacology*
  • Topoisomerase I Inhibitors*

Substances

  • Enzyme Inhibitors
  • Nitriles
  • Topoisomerase I Inhibitors
  • benzonitrile
  • Camptothecin