Discovery of 4-Amino and 4-Hydroxy-1-aroylindoles as Potent Tubulin Polymerization Inhibitors

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• 作者：Jing-Ping Liou ; Zi-Yi Wu ; Ching-Chuan Kuo ; Chi-Yen Chang ; Pei-Yi Lu ; Chi-Ming Chen ; Hsing-Pang Hsieh ; Jang-Yang Chang
• 刊名：Journal of Medicinal Chemistry
• 出版年：2008
• 出版时间：July 24, 2008
• 年：2008
• 卷：51
• 期：14
• 页码：4351-4355
• 全文大小：181K
• 年卷期：v.51,no.14(July 24, 2008)
• ISSN：1520-4804

文摘

1-Aroylindoline, 1-aroyl-1,2,3,4-tetrahydroquinoline, and 1-aroylindole derivatives were synthesized and evaluated for anticancer activity. The 4-amino and 4-hydroxy-1-aroylindoles 26 and 27 with IC₅₀ of 0.9 and 0.6 μM, respectively, exhibited antitubulin activity superior or comparable to that of colchicine and combretastatin A-4. They also showed antiproliferative activity with IC₅₀ of 0.3−5.4 nM in a set of human cancer cell lines.