國家衛生研究院 NHRI:Item 3990099045/4280
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    题名: 5-Amino-2-Aroylquinolines as Highly Potent Tubulin Polymerization Inhibitors
    作者: Nien, CY;Chen, YC;Kuo, CC;Hsieh, HP;Chang, CY;Wu, JS;Wu, SY;Liou, JP;Chang, JY
    贡献者: National Institute of Cancer Research;Division of Biotechnology and Pharmaceutical Research
    摘要: 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 mu M) exhibited more potent inhibition of tubulin polymerization than 1a (IC50 = 2.1 mu M) and showed strong binding property to the colchicine binding site of microtubules.
    日期: 2010-03-11
    關聯: Journal of Medicinal Chemistry. 2010 Mar 11;53(5):2309-2313.
    Link to: http://dx.doi.org/10.1021/jm900685y
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0022-2623&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000275087000036
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=77949378899
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