| Design, Synthesis and Pharmacological Evaluation of Novel 4-Phenoxyquinoline Derivatives as Potential Antitumor Agents | |
| Alternative Title | Design, Synthesis and Pharmacological Evaluation of Novel 4-Phenoxyquinoline Derivatives as Potential Antitumor Agents |
| Hu Hao1; Jiang Mingyan1; Xie Lijun2; Hu Gang1; Zhang Cuirong1; Zhang Lixia1; Zhou Shunguang1; Zhang Meihui1; Gong Ping1 | |
| 2015 | |
| Source Publication | CHEMICAL RESEARCH IN CHINESE UNIVERSITIES
 |
| ISSN | 1005-9040 |
| Volume | 31Issue:5Pages:746-755 |
| 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 IC50 values of 0.04, 0.09, 0.67, 0.39 and 1.10 mu mol/L against HT-29, H460, A549, MKN-45 and U87MG cell lines, respectively. |
| Other 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_(50) 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. |
| Keyword | MET KINASE INHIBITORS GROWTH-FACTOR RECEPTOR C-MET 6,7-DISUBSTITUTED-4-PHENOXYQUINOLINE DERIVATIVES BIOLOGICAL EVALUATION DISCOVERY MOIETY BEARING IDENTIFICATION 4-Phenoxyquinoline derivative Cytotoxic activity 3-Amino-2-cyano-acrylamide |
| Indexed By | CSCD |
| Language | 英语 |
| Funding Project | [Program for Liaoning Innovative Research Team in University, China] |
| CSCD ID | CSCD:5537994 |
| Citation statistics | |
| Document Type | 期刊论文 |
| Identifier | http://ir.imr.ac.cn/handle/321006/144766 |
| Collection | 中国科学院金属研究所 |
| Affiliation | 1.中国科学院金属研究所 2.Fujian Institute Microbiol, Fuzhou 350007, Peoples R China |
| Recommended Citation GB/T 7714 | Hu Hao,Jiang Mingyan,Xie Lijun,et al. Design, Synthesis and Pharmacological Evaluation of Novel 4-Phenoxyquinoline Derivatives as Potential Antitumor Agents[J]. CHEMICAL RESEARCH IN CHINESE UNIVERSITIES,2015,31(5):746-755. |
| APA | Hu Hao.,Jiang Mingyan.,Xie Lijun.,Hu Gang.,Zhang Cuirong.,...&Gong Ping.(2015).Design, Synthesis and Pharmacological Evaluation of Novel 4-Phenoxyquinoline Derivatives as Potential Antitumor Agents.CHEMICAL RESEARCH IN CHINESE UNIVERSITIES,31(5),746-755. |
| MLA | Hu Hao,et al."Design, Synthesis and Pharmacological Evaluation of Novel 4-Phenoxyquinoline Derivatives as Potential Antitumor Agents".CHEMICAL RESEARCH IN CHINESE UNIVERSITIES 31.5(2015):746-755. |
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