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 microM, which is five times that of camptothecin from the results of agarose gel electrophoresis.
Lin
C F
CF
School of Chemistry, Kaohsiung Medical University, Kaohsiung, Taiwan.
Hsieh
P C
PC
Lu
W D
WD
Chiu
H F
HF
Wu
M J
MJ
D002166:Camptothecin / Q000494:pharmacology; D004587:Electrophoresis, Agar Gel; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D009570:Nitriles / Q000494:pharmacology*; D059004:Topoisomerase I Inhibitors
D004791:Enzyme Inhibitors; D009570:Nitriles; D059004:Topoisomerase I Inhibitors; C014356:benzonitrile; D002166:Camptothecin