5-Amino-2-Aroylquinolines as highly potent tubulin polymerization inhibitors

Chih Ying Nien, Yun Ching Chen, Ching Chuan Kuo, Hsing Pang Hsieh, Chi Yen Chang, Jian Sung Wu, Su Ying Wu, Jing Ping Liou, Jang Yang Chang

研究成果: 雜誌貢獻文章同行評審

66 引文 斯高帕斯(Scopus)

摘要

A series of aroylquinoline derivatives were synthesized and evaluated for anticancer activity. 5-Amino6-methoxy-2-aroylquinoline 15 showed more potent antiproliferative activity (IC50 values ranging from 0.2 to 0.4 nM) as compared to la (combretastatin A-4) (IC50 = 1-9-835 nM) against various human cancer cell lines and a MDR-resistant cancer cell line. Compound 15 (IC50 = 1-6 μM) exhibited more potent inhibition of tubulin polymerization than la (IC50 = 2.1 μM) and showed strong binding property to the colchicine binding site of microtubules.

原文英語
頁(從 - 到)2309-2313
頁數5
期刊Journal of Medicinal Chemistry
53
發行號5
DOIs
出版狀態已發佈 - 三月 11 2010

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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