Synthesis and cytotoxicity of analogues of the antibiotic BE 10988 inhibitors of DNA topoisomerase II.
Indolequinone derivatives of the antitumour antibiotic BE 10988 were synthesized and evaluated for their cytotoxicity and action mechanism. The quinone system is essential to biological activity and the thiazole ring plays a major role in the poisoning of topoisomerase II.
Catrycke
M O
MO
Institut de Chimie Pharmaceutique, Université de Lille 2, France.
Houssin
R
R
Hénichart
J P
JP
Pfeiffer
B
B
Renard
P
P
Dassonneville
L
L
Bailly
C
C
D000818:Animals; D002455:Cell Division / Q000187:drug effects; D004247:DNA / Q000378:metabolism; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*; D007211:Indoles / Q000737:chemistry; D020128:Inhibitory Concentration 50; D007939:Leukemia L1210 / Q000188:drug therapy; D051379:Mice; D011809:Quinones / Q000737:chemistry; D012995:Solubility; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000737:chemistry*; D059005:Topoisomerase II Inhibitors
D004791:Enzyme Inhibitors; D007211:Indoles; D011809:Quinones; D013844:Thiazoles; D059005:Topoisomerase II Inhibitors; C069638:BE 10988; D004247:DNA