Antitumor agents. 192. Antitubulin effect and cytotoxicity of C(7)-oxygenated allocolchicinoids
Two allocolchicinoids 6 and 8, prepared from colchicine, together with allo compounds 9-11, made from 6 by reduction and regiodemethylation, were evaluated for antitubulin and antitumor activities. Structures of 6, 8, and 10 were confirmed by X-ray crystallographic analysis. Compounds 6, 8, and 9 have high tubulin binding affinity and display potent inhibitory activities against tubulin polymerization and solid human tumor cell lines. Particularly, drug-resistant KB cell lines, including KB-7d, KB-VCR, and KB-CPT, do not show marked resistance to these compounds.
Guan, J; Zhu, XK; Brossi, A; Tachibana, Y; Bastow, KF; Verdier-Pinard, P; Hamel, E; McPhail, AT; Lee, KH
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