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

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60 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

ASJC Scopus subject areas

  • Organic Chemistry

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    Liou, J. P., Wu, Z. Y., Kuo, C. C., Chang, C. Y., Lu, P. Y., Chen, C. M., Hsieh, H. P., & Chang, J. Y. (2008). Discovery of 4-amino and 4-hydroxy-1-aroylindoles as potent tubulin polymerization inhibitors. Journal of Medicinal Chemistry, 51(14), 4351-4355. https://doi.org/10.1021/jm800150d