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

85 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 - 2010 Mar 11

UN SDGs

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

SDG 3 Good Health and Well-being

All Science Journal Classification (ASJC) codes

Molecular Medicine
Drug Discovery

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10.1021/jm900685y

Cite this

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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\}",

year = "2010",

month = mar,

day = "11",

doi = "10.1021/jm900685y",

language = "English",

volume = "53",

pages = "2309--2313",

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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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U2 - 10.1021/jm900685y

DO - 10.1021/jm900685y

M3 - Article

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AN - SCOPUS:77949378899

SN - 0022-2623

VL - 53

SP - 2309

EP - 2313

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

IS - 5

ER -

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

Abstract

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