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

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

    Fingerprint

ASJC Scopus subject areas

  • Organic Chemistry

Cite this

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