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
其他题名	Design, Synthesis and Pharmacological Evaluation of Novel 4-Phenoxyquinoline Derivatives as Potential Antitumor Agents
	Hu Hao 1; Jiang Mingyan 1; Xie Lijun 2; Hu Gang 1; Zhang Cuirong 1; Zhang Lixia 1; Zhou Shunguang 1; Zhang Meihui 1; Gong Ping 1
	2015
发表期刊	CHEMICAL RESEARCH IN CHINESE UNIVERSITIES
ISSN	1005-9040
卷号	31 期号:5 页码:746-755
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 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.
其他摘要	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 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.
关键词	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
收录类别	CSCD
语种	英语
资助项目	[Program for Liaoning Innovative Research Team in University, China]
CSCD记录号	CSCD:5537994
引用统计	被引频次：4[CSCD] [CSCD记录]
文献类型	期刊论文
条目标识符	http://ir.imr.ac.cn/handle/321006/144766
专题	中国科学院金属研究所
作者单位	1.中国科学院金属研究所 2.Fujian Institute Microbiol, Fuzhou 350007, Peoples R China
推荐引用方式 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.