2-(6-Aryl-3(Z)-hexen-1,5-diynyl)anilines as a New Class of Potent Antitubulin Agents

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• 作者：Yu-Hsiang Lo ; Ching-Chih Lin ; Chi-Fong Lin ; Ying-Ting Lin ; Tsai-Hui Duh ; Yi-Ren Hong ; Sheng-Huei Yang ; Shinne-Ren Lin ; Shyh-Chyun Yang ; Long-Sen Chang ; Ming-Jung Wu
• 刊名：Journal of Medicinal Chemistry
• 出版年：2008
• 出版时间：May 8, 2008
• 年：2008
• 卷：51
• 期：9
• 页码：2682 - 2688
• 全文大小：1006K
• 年卷期：v.51,no.9(May 8, 2008)
• ISSN：1520-4804

文摘

Compounds 2a−h and 6 displayed significant GI₅₀ values of 10⁻⁷−10⁻⁶ M against various cancer cell lines. Of these compounds, 2-(6-(2-trifluoromethylphenyl))-3(Z)-hexen-1,5-diynyl)aniline (2c) showed the most potent growth inhibition activity. Compound 2c also arrested cancer cells in the G2/M phase and in low concentration reduced a significant percentage of MDA-MB-231/ATCC breast cancer tetraploid cells. In addition to the G2/M block, compound 2c caused microtubule depolymerization and induced apoptosis via activation of the caspase family.