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5-Amino-2-Aroylquinolines as Highly Potent Tubulin Polymerization Inhibitors

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journal contribution
posted on 2010-03-11, 00:00 authored by 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
A series of aroylquinoline derivatives were synthesized and evaluated for anticancer activity. 5-Amino-6-methoxy-2-aroylquinoline 15 showed more potent antiproliferative activity (IC50 values ranging from 0.2 to 0.4 nM) as compared to 1a (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 1a (IC50 = 2.1 μM) and showed strong binding property to the colchicine binding site of microtubules.