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

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65 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)2309-2313
Number of pages5
JournalJournal of Medicinal Chemistry
Volume53
Issue number5
DOIs
Publication statusPublished - Mar 11 2010

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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    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