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

Research output: Contribution to journalArticle

58 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)4351-4355
Number of pages5
JournalJournal of Medicinal Chemistry
Volume51
Issue number14
DOIs
Publication statusPublished - Jul 24 2008

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Tubulin Modulators
Colchicine
Inhibitory Concentration 50
Cells
Derivatives
Cell Line
Neoplasms
fosbretabulin
1,2,3,4-tetrahydroquinoline

ASJC Scopus subject areas

  • Organic Chemistry

Cite this

Discovery of 4-amino and 4-hydroxy-1-aroylindoles as potent tubulin polymerization inhibitors. / Liou, Jing Ping; Wu, Zi Yi; Kuo, Ching Chuan; Chang, Chi Yen; Lu, Pei Yi; Chen, Chi Ming; Hsieh, Hsing Pang; Chang, Jang Yang.

In: Journal of Medicinal Chemistry, Vol. 51, No. 14, 24.07.2008, p. 4351-4355.

Research output: Contribution to journalArticle

Liou, JP, Wu, ZY, Kuo, CC, Chang, CY, Lu, PY, Chen, CM, Hsieh, HP & Chang, JY 2008, 'Discovery of 4-amino and 4-hydroxy-1-aroylindoles as potent tubulin polymerization inhibitors', Journal of Medicinal Chemistry, vol. 51, no. 14, pp. 4351-4355. https://doi.org/10.1021/jm800150d
Liou, Jing Ping ; Wu, Zi Yi ; Kuo, Ching Chuan ; Chang, Chi Yen ; Lu, Pei Yi ; Chen, Chi Ming ; Hsieh, Hsing Pang ; Chang, Jang Yang. / Discovery of 4-amino and 4-hydroxy-1-aroylindoles as potent tubulin polymerization inhibitors. In: Journal of Medicinal Chemistry. 2008 ; Vol. 51, No. 14. pp. 4351-4355.
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