5-Amino-2-Aroylquinolines as Highly Potent Tubulin Polymerization Inhibitors
Journal of Medicinal Chemistry2010Vol. 53(5), pp. 2309–2313
Citations Over TimeTop 10% of 2010 papers
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
Abstract
A series of aroylquinoline derivatives were synthesized and evaluated for anticancer activity. 5-Amino-6-methoxy-2-aroylquinoline 15 showed more potent antiproliferative activity (IC(50) values ranging from 0.2 to 0.4 nM) as compared to 1a (combretastatin A-4) (IC(50) = 1.9-835 nM) against various human cancer cell lines and a MDR-resistant cancer cell line. Compound 15 (IC(50) = 1.6 microM) exhibited more potent inhibition of tubulin polymerization than 1a (IC(50) = 2.1 microM) and showed strong binding property to the colchicine binding site of microtubules.
Related Papers
- → Colchicine and the Heart(2013)158 cited
- → Design, synthesis and biological evaluation of quinoline-indole derivatives as anti-tubulin agents targeting the colchicine binding site(2018)84 cited
- → Design and Synthesis of Cyclopropylamide Analogues of Combretastatin-A4 as Novel Microtubule-Stabilizing Agents(2013)62 cited
- → The effect of colchicine on pyrin and pyrin interacting proteins(2012)42 cited
- → Resistance of Rosa microtubule polymerization to colchicine results from a low-affinity interaction of colchicine and tubulin(1987)51 cited