Design, Synthesis and Cytotoxicity of Novel 2-Arylvinyl-4-aminoquinoline Derivatives
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概要
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With an aim to develop promising anti-tumor agents, a novel series of 2-arylvinyl-4-aminoquinoline derivatives were designed, synthesized and evaluated for their cytotoxicity against H-460, HT-29, HepG2 and SGC-7901 cell lines in vitro. The pharmacological results indicated that most compounds were more potent than the positive controls, especially compounds 8, 14 and 16 with IC50 values ranging from 0.05 to 0.85 µM against all tested cell lines respectively, which were 5.7- to 112-fold better than Iressa. The most active compound 14 (IC50 values of 0.05, 0.25, 0.16, 0.68 µM), bearing 4-fluorostyryl at C-2 position and 3-(dimethylamino)-1-propylamino at C-4 position, showed great promise as a lead for the development of more effective quinoline analogues.
著者
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Zhai Xin
Key Lab Of New Drugs Design And Discovery Of Liaoning Province School Of Pharmaceutical Engineering
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Gong Ping
Key Lab Of New Drugs Design And Discovery Of Liaoning Province School Of Pharmaceutical Engineering
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Liang Chuang
Key Lab of New Drugs Design and Discovery of Liaoning Province, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University
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Chen Zhichao
Key Lab of New Drugs Design and Discovery of Liaoning Province, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University
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Jiang Nan
Key Lab of New Drugs Design and Discovery of Liaoning Province, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University
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Sun Chao
Key Lab of New Drugs Design and Discovery of Liaoning Province, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University
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Han Jing
Key Lab of New Drugs Design and Discovery of Liaoning Province, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University
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