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

研究成果: 雜誌貢獻 › 文章 › 同行評審

62 引文斯高帕斯（Scopus）

摘要

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.

原文	英語
頁（從 - 到）	4351-4355
頁數	5
期刊	Journal of Medicinal Chemistry
卷	51
發行號	14
DOIs	https://doi.org/10.1021/jm800150d
出版狀態	已發佈 - 七月 24 2008

ASJC Scopus subject areas

Organic Chemistry

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10.1021/jm800150d

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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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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

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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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