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

doi:10.1021/jm800150d

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 journal › Article › peer-review

69 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 language	English
Pages (from-to)	4351-4355
Number of pages	5
Journal	Journal of Medicinal Chemistry
Volume	51
Issue number	14
DOIs	https://doi.org/10.1021/jm800150d
Publication status	Published - Jul 24 2008

ASJC Scopus subject areas

Organic Chemistry

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10.1021/jm800150d

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title = "Discovery of 4-amino and 4-hydroxy-1-aroylindoles as potent tubulin polymerization inhibitors",

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.",

author = "Liou, {Jing Ping} and Wu, {Zi Yi} and Kuo, {Ching Chuan} and Chang, {Chi Yen} and Lu, {Pei Yi} and Chen, {Chi Ming} and Hsieh, {Hsing Pang} and Chang, {Jang Yang}",

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doi = "10.1021/jm800150d",

language = "English",

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T1 - Discovery of 4-amino and 4-hydroxy-1-aroylindoles as potent tubulin polymerization inhibitors

AU - Liou, Jing Ping

AU - Wu, Zi Yi

AU - Kuo, Ching Chuan

AU - Chang, Chi Yen

AU - Lu, Pei Yi

AU - Chen, Chi Ming

AU - Hsieh, Hsing Pang

AU - Chang, Jang Yang

PY - 2008/7/24

Y1 - 2008/7/24

N2 - 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.

AB - 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.

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Discovery of 4-amino and 4-hydroxy-1-aroylindoles as potent tubulin polymerization inhibitors

Abstract

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