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

Research output: Contribution to journalArticle

60 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

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Tubulin Modulators
Inhibitory Concentration 50
Cell Line
Colchicine
Tubulin
Microtubules
Polymerization
Neoplasms
Binding Sites

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

Cite this

Nien, C. Y., Chen, Y. C., Kuo, C. C., Hsieh, H. P., Chang, C. Y., Wu, J. S., ... 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

5-Amino-2-Aroylquinolines as highly potent tubulin polymerization inhibitors. / Nien, Chih Ying; Chen, Yun Ching; Kuo, Ching Chuan; Hsieh, Hsing Pang; Chang, Chi Yen; Wu, Jian Sung; Wu, Su Ying; Liou, Jing Ping; Chang, Jang Yang.

In: Journal of Medicinal Chemistry, Vol. 53, No. 5, 11.03.2010, p. 2309-2313.

Research output: Contribution to journalArticle

Nien, CY, Chen, YC, Kuo, CC, Hsieh, HP, Chang, CY, Wu, JS, Wu, SY, Liou, JP & Chang, JY 2010, '5-Amino-2-Aroylquinolines as highly potent tubulin polymerization inhibitors', Journal of Medicinal Chemistry, vol. 53, no. 5, pp. 2309-2313. https://doi.org/10.1021/jm900685y
Nien, Chih Ying ; Chen, Yun Ching ; Kuo, Ching Chuan ; Hsieh, Hsing Pang ; Chang, Chi Yen ; Wu, Jian Sung ; Wu, Su Ying ; Liou, Jing Ping ; Chang, Jang Yang. / 5-Amino-2-Aroylquinolines as highly potent tubulin polymerization inhibitors. In: Journal of Medicinal Chemistry. 2010 ; Vol. 53, No. 5. pp. 2309-2313.
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