Design, synthesis, biochemical, and biological evaluation of nitrogen-containing trifluoro structural modifications of combretastatin A-4

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• 作者：John J. Hall ; Madhavi Sriram ; Tracy E. Strecker ; Justin K. Tidmore ; Christopher J. Jelinek ; G.D. Kishore Kumar ; Mallinath B. Hadimani ; George R. Pettit ; David J. Chaplin ; Mary Lynn Trawick ; Kevin G. P
• 关键词：Combretastatin ; Inhibitors of tubulin assembly ; Anti-cancer agents
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2008
• 出版时间：15 September 2008
• 年：2008
• 卷：18
• 期：18
• 页码：5146-5149
• 全文大小：169 K

文摘

A new trifluorinated amino-combretastatin analogue, (Z)-2-(4′-methoxy-3′-aminophenyl)-1-(3,4,5-trifluorophenyl)ethene, prepared by chemical synthesis, was found to be a potent inhibitor of tubulin assembly (IC₅₀ = 2.9 μM), and cytotoxic against selected human cancer cell lines. This new lead compound is among the most active from a group of related structural modifications.