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Design, synthesis and pharmacological evaluation of novel 4-phenoxyquinoline derivatives as potential antitumor agents

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Design, synthesis and pharmacological evaluation of novel 4-phenoxyquinoline derivatives as potential antitumor agents

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作者
Hao Hu;Mingyan Jiang;Lijun Xie;Gang Hu;Cuirong Zhang;Lixia Zhang;Shunguang Zhou;Meihui Zhang;Ping Gong*
刊物名称
Chemical Research in Chinese Universities
2015
31
5
746-755

{Author}: Hao Hu;Mingyan Jiang;Lijun Xie;Gang Hu;Cuirong Zhang;Lixia Zhang;Shunguang Zhou;Meihui Zhang;Ping Gong*

{Journal}: Chemical Research in Chinese Universities

{Year}: 2015

{Volume}: 31

{Issue}: 5

{Pages}:746-755

{Keywords}: 4-Phenoxyquinoline derivative;Cytotoxic activity;3-Amino-2-cyano-acrylamide

{Abstract}: A series of novel 4-phenoxyquinoline derivatives containing 3-amino-2-cyano-acrylamide framework was designed and synthesized, and the in vitro cytotoxic activities of them against five cancer cell lines(HT-29, H460, A549, MKN-45, and U87MG) were evaluated. Most of the compounds exhibited moderate-to-significant cytotoxicity and high selectivity against one or more cell lines as compared with Foretinib. The studies of their preliminary structure-activity relationships(SARs) indicate that the compounds containing methyl groups, especially methyl groups at 4-position of the phenyl ring(moiety B) are more effective. Among them, compound 36 shows the most potent antitumor activities with IC<sub>50</sub> values of 0.04, 0.09, 0.67, 0.39 and 1.10 μmol/L against HT-29, H460, A549, MKN-45 and U87MG cell lines, respectively.

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