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

doi:10.1021/jm070557q

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

Research output: Contribution to journal › Article › peer-review

64 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 language	English
Pages (from-to)	4548-4552
Number of pages	5
Journal	Journal of Medicinal Chemistry
Volume	50
Issue number	18
DOIs	https://doi.org/10.1021/jm070557q
Publication status	Published - Sept 6 2007

ASJC Scopus subject areas

Molecular Medicine
Drug Discovery

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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.",

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AU - Liou, Jing Ping

AU - Wu, Chang Ying

AU - Hsieh, Hsing Pang

AU - Chang, Chi Yen

AU - Chen, Chi Ming

AU - Kuo, Ching Chuan

AU - Chang, Jang Yang

PY - 2007/9/6

Y1 - 2007/9/6

N2 - 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.

AB - 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.

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

Abstract

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