Discovery of 4-amino and 4-hydroxy-1-aroylindoles as potent tubulin polymerization inhibitors

Jing Ping Liou, Zi Yi Wu, Ching Chuan Kuo, Chi Yen Chang, Pei Yi Lu, Chi Ming Chen, Hsing Pang Hsieh, Jang Yang Chang

研究成果: 雜誌貢獻文章同行評審

62 引文 斯高帕斯(Scopus)

摘要

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.

原文英語
頁(從 - 到)4351-4355
頁數5
期刊Journal of Medicinal Chemistry
51
發行號14
DOIs
出版狀態已發佈 - 七月 24 2008

ASJC Scopus subject areas

  • Organic Chemistry

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