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  • Title: 5-Amino-2-aroylquinolines as highly potent tubulin polymerization inhibitors.
    Author: Nien CY, Chen YC, Kuo CC, Hsieh HP, Chang CY, Wu JS, Wu SY, Liou JP, Chang JY.
    Journal: J Med Chem; 2010 Mar 11; 53(5):2309-13. PubMed ID: 20148562.
    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.
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