Antitumor agents. 192. Antitubulin effect and cytotoxicity of C(7)-oxygenated allocolchicinoids

Authors
Guan, J Zhu, XK Brossi, A Tachibana, Y Bastow, KF Verdier-Pinard, P Hamel, E McPhail, AT Lee, KH
Citation
J. Guan et al., Antitumor agents. 192. Antitubulin effect and cytotoxicity of C(7)-oxygenated allocolchicinoids, COLL CZECH, 64(2), 1999, pp. 217-228
Citations number
23
Categorie Soggetti
Chemistry
Journal title
COLLECTION OF CZECHOSLOVAK CHEMICAL COMMUNICATIONS
ISSN journal
00100765 → ACNP
Volume
64
Issue
2
Year of publication
1999
Pages
217 - 228
Database
ISI
SICI code
0010-0765(199902)64:2<217:AA1AEA>2.0.ZU;2-Z
Abstract
Two allocolchicinoids 6 and 8, prepared from colchicine, together with allo compounds 9-11, made from 6 by reduction and regiodemethylation, were eval uated for antitubulin and antitumor activities. Structures of 6, 8, and 10 were confirmed by X-ray crystallographic analysis. Compounds 6, 8, and 9 ha ve high tubulin binding affinity and display potent inhibitory activities a gainst tubulin polymerization and solid human tumor cell lines. Particularl y, drug-resistant KB cell lines, including KB-7d, KB-VCR, and KB-CPT, do no t show marked resistance to these compounds.