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

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

82 Citations (Scopus)

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.

Original language	English
Pages (from-to)	2309-2313
Number of pages	5
Journal	Journal of Medicinal Chemistry
Volume	53
Issue number	5
DOIs	https://doi.org/10.1021/jm900685y
Publication status	Published - Mar 11 2010

ASJC Scopus subject areas

Molecular Medicine
Drug Discovery

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This output contributes to the following UN Sustainable Development Goals (SDGs)

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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.",

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

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doi = "10.1021/jm900685y",

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T1 - 5-Amino-2-Aroylquinolines as highly potent tubulin polymerization inhibitors

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

Abstract

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