5-Amino-2-Aroylquinolines as highly potent tubulin polymerization inhibitors

Chih Ying Nien; Yun Ching Chen; Ching Chuan Kuo; Hsing Pang Hsieh; Chi Yen Chang; Jian Sung Wu; Su Ying Wu; Jing Ping Liou; Jang Yang Chang

doi:10.1021/jm900685y

5-Amino-2-Aroylquinolines as highly potent tubulin polymerization inhibitors

Chih Ying Nien, Yun Ching Chen, Ching Chuan Kuo, Hsing Pang Hsieh, Chi Yen Chang, Jian Sung Wu, Su Ying Wu, Jing Ping Liou, Jang Yang Chang

研究成果: Article › 同行評審

82 引文斯高帕斯（Scopus）

摘要

A series of aroylquinoline derivatives were synthesized and evaluated for anticancer activity. 5-Amino6-methoxy-2-aroylquinoline 15 showed more potent antiproliferative activity (IC₅₀ values ranging from 0.2 to 0.4 nM) as compared to la (combretastatin A-4) (IC₅₀ = 1-9-835 nM) against various human cancer cell lines and a MDR-resistant cancer cell line. Compound 15 (IC₅₀ = 1-6 μM) exhibited more potent inhibition of tubulin polymerization than la (IC₅₀ = 2.1 μM) and showed strong binding property to the colchicine binding site of microtubules.

原文	English
頁（從 - 到）	2309-2313
頁數	5
期刊	Journal of Medicinal Chemistry
卷	53
發行號	5
DOIs	https://doi.org/10.1021/jm900685y
出版狀態	Published - 2010 3月 11

All Science Journal Classification (ASJC) codes

分子醫學
藥物發現

UN SDG

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10.1021/jm900685y

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title = "5-Amino-2-Aroylquinolines as highly potent tubulin polymerization inhibitors",

abstract = "A series of aroylquinoline derivatives were synthesized and evaluated for anticancer activity. 5-Amino6-methoxy-2-aroylquinoline 15 showed more potent antiproliferative activity (IC50 values ranging from 0.2 to 0.4 nM) as compared to la (combretastatin A-4) (IC50 = 1-9-835 nM) against various human cancer cell lines and a MDR-resistant cancer cell line. Compound 15 (IC50 = 1-6 μM) exhibited more potent inhibition of tubulin polymerization than la (IC50 = 2.1 μM) and showed strong binding property to the colchicine binding site of microtubules.",

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AU - Nien, Chih Ying

AU - Chen, Yun Ching

AU - Kuo, Ching Chuan

AU - Hsieh, Hsing Pang

AU - Chang, Chi Yen

AU - Wu, Jian Sung

AU - Wu, Su Ying

AU - Liou, Jing Ping

AU - Chang, Jang Yang

PY - 2010/3/11

Y1 - 2010/3/11

N2 - A series of aroylquinoline derivatives were synthesized and evaluated for anticancer activity. 5-Amino6-methoxy-2-aroylquinoline 15 showed more potent antiproliferative activity (IC50 values ranging from 0.2 to 0.4 nM) as compared to la (combretastatin A-4) (IC50 = 1-9-835 nM) against various human cancer cell lines and a MDR-resistant cancer cell line. Compound 15 (IC50 = 1-6 μM) exhibited more potent inhibition of tubulin polymerization than la (IC50 = 2.1 μM) and showed strong binding property to the colchicine binding site of microtubules.

AB - A series of aroylquinoline derivatives were synthesized and evaluated for anticancer activity. 5-Amino6-methoxy-2-aroylquinoline 15 showed more potent antiproliferative activity (IC50 values ranging from 0.2 to 0.4 nM) as compared to la (combretastatin A-4) (IC50 = 1-9-835 nM) against various human cancer cell lines and a MDR-resistant cancer cell line. Compound 15 (IC50 = 1-6 μM) exhibited more potent inhibition of tubulin polymerization than la (IC50 = 2.1 μM) and showed strong binding property to the colchicine binding site of microtubules.

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5-Amino-2-Aroylquinolines as highly potent tubulin polymerization inhibitors

摘要

All Science Journal Classification (ASJC) codes

UN SDG

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