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