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Design, Synthesis and Pharmacological Evaluation of Novel 4-Phenoxyquinoline Derivatives as Potential Antitumor Agents
Alternative TitleDesign, 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 PublicationCHEMICAL RESEARCH IN CHINESE UNIVERSITIES
ISSN1005-9040
Volume31Issue:5Pages:746-755
AbstractA 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 AbstractA 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.
KeywordMET 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 ByCSCD
Language英语
Funding Project[Program for Liaoning Innovative Research Team in University, China]
CSCD IDCSCD:5537994
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Document Type期刊论文
Identifierhttp://ir.imr.ac.cn/handle/321006/144766
Collection中国科学院金属研究所
Affiliation1.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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