Design, Synthesis and Pharmacological Evaluation of Novel 4-Phenoxyquinoline Derivatives as Potential Antitumor Agents  

作　　者：HU Hao JIANG Mingyan XIE Lijun HU Gang ZHANG Cuirong ZHANG Lixia ZHOU Shunguang ZHANG Meihui GONG Ping 

机构地区：[1]Key Laboratory of Structure-based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, R R. China [2]Fujian Institute of Microbiology, Fuzhou 350007, P R. China

出　　处：《Chemical Research in Chinese Universities》2015年第5期746-755,共10页高等学校化学研究（英文版）

摘　　要：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 anti- tumor activities with IC50 values of 0.04, 0.09, 0.67, 0.39 and l. 10 μmol/L against HT-29, H460, A549, MKN-45 and U87MG cell lines, respectively.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 anti- tumor activities with IC50 values of 0.04, 0.09, 0.67, 0.39 and l. 10 μmol/L against HT-29, H460, A549, MKN-45 and U87MG cell lines, respectively.

关 键 词：4-Phenoxyquinoline derivative Cytotoxic activity 3-Amino-2-cyano-acrylamide 

分 类 号：Q939.117[生物学—微生物学] O641.4[理学—物理化学]