期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 53, 期 5, 页码 2309-2313出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm900685y
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资金
- National Science Council of the Republic of China [NSC 98-2323-B-038-003, NSC 98-2113-M-038-002-MY2, NSC 96-2752-B-400-001-PAE]
- Center of Excellence for Clinical Trial and Research in Neurology and Neurosurgery, Taiwan [DOH-TD-13-111-002]
- National Health Research Institutes, Taiwan [CA-097-PP-02]
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.
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