Interactions of long-chain homologues of colchicine with tubulin

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• 作者：Ana Marzo-Mas^a ; Pascale Barbier^b ; Gilles Breuzard^b ; Diane Allegro^b ; Eva Falomir^a ; Juan Murga^a ; ^{jmurga@uji.es} ; Miguel Carda^a ; Vincent Peyrot^b ; ^{vincent.peyrot@univ-amu.fr} ; J. Alberto Marco^c
• 关键词：Tubulin ; Colchicine ; Microtubules ; Abnormal polymerization ; Cytotoxicity ; Docking studies
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：27 January 2017
• 年：2017
• 卷：126
• 期：Complete
• 页码：526-535
• 全文大小：2140 K
• 卷排序：126

文摘

Several N-acyl colchicine analogues have been synthesized. Their cytotoxicities and ability to inhibit microtubule assembly have been measured. Some of them exhibit activities in the picomolar range against the HT-29 line. Some of the compounds induce the formation of abnormal polymers. Some of them bind concomitantly to β-tubulin and to the neighboring α-tubulin.