4- And 5-aroylindoles as novel classes of potent antitubulin agents

Jing Ping Liou, Chang Ying Wu, Hsing Pang Hsieh, Chi Yen Chang, Chi Ming Chen, Ching Chuan Kuo, Jang Yang Chang

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57 Citations (Scopus)

Abstract

A novel series of 4- and 5-aroylindole derivatives was prepared and evaluated for antitumor activity. Several compounds showed excellent antiproliferative activity as inhibitors of tubulin polymerization. Compounds 13,14,15, and 18, with IC50 values of 1.9, 1.1, 1.2, and 1.8 μM, respectively, exhibited more potent inhibition of tubulin polymerization than colchicine. They also displayed antiproliferative activity, with IC50 values ranging from 10 to 43 nM in a variety of human cell lines from different organs.

Original languageEnglish
Pages (from-to)4548-4552
Number of pages5
JournalJournal of Medicinal Chemistry
Volume50
Issue number18
DOIs
Publication statusPublished - Sep 6 2007

ASJC Scopus subject areas

  • Organic Chemistry

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  • Cite this

    Liou, J. P., Wu, C. Y., Hsieh, H. P., Chang, C. Y., Chen, C. M., Kuo, C. C., & Chang, J. Y. (2007). 4- And 5-aroylindoles as novel classes of potent antitubulin agents. Journal of Medicinal Chemistry, 50(18), 4548-4552. https://doi.org/10.1021/jm070557q