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: Article

63 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English
頁(從 - 到)2309-2313
頁數5
期刊Journal of Medicinal Chemistry
53
發行號5
DOIs
出版狀態Published - 2010 三月 11

    指紋

All Science Journal Classification (ASJC) codes

  • Molecular Medicine
  • Drug Discovery

引用此

Nien, C. Y., Chen, Y. C., Kuo, C. C., Hsieh, H. P., Chang, C. Y., Wu, J. S., Wu, S. Y., Liou, J. P., & Chang, J-Y. (2010). 5-Amino-2-Aroylquinolines as highly potent tubulin polymerization inhibitors. Journal of Medicinal Chemistry, 53(5), 2309-2313. https://doi.org/10.1021/jm900685y