Synthesis, Anticancer and Antibacterial Activities of Novel 2-Amino-4-phenylthiazole Derivatives Containing Amide Moiety

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	Synthesis, Anticancer and Antibacterial Activities of Novel 2-Amino-4-phenylthiazole Derivatives Containing Amide Moiety
	Zhang Zhihua 3; Chen Yu 3; Chai Baoshan 3; Yang Xiaoman 1; Cai Xiaoyu 1; Cui Bo 1; You Song 3
刊名	CHINESE JOURNAL OF ORGANIC CHEMISTRY
	2017
卷号	37 期号:9 页码:2377-2384
关键词	BIOLOGICAL EVALUATION KINASE INHIBITORS SORAFENIB ANALOGS ANTITUMOR AGENTS RATIONAL DESIGN 2-AMINOTHIAZOLES BRAF MELANOMA THIOUREA GROWTH thiazole derivative amide synthesis anticancer antibacterial
ISSN号	0253-2786
其他题名	Synthesis, Anticancer and Antibacterial Activities of Novel 2-Amino-4-phenylthiazole Derivatives Containing Amide Moiety
英文摘要	A series of novel 2-amino-4-phenylthiazole derivatives containing amide moiety were designed and synthesized based on the structural features of sorafenib. The structures of synthesized compounds were characterized by H-1 NMR, C-13 NMR and HRMS. Both the anticancer and antibacterial activities of all the target compounds were evaluated. Most of the compounds showed potent activities, especially N-(3-(2-acetamidothiazol-4-yl) phenyl)-3-fluorobenzamide (4n) exhibited a remarkable antitumor effect against human colon cancer cell line (HT29) and human lung epithelial cells (A549) cells with IC50 values of 6.31 and 7.98 mu mol circle L-1, respectively. Further mechanistic study revealed that 4n can influence the Raf/MEK/ ERK pathway. In addition, N-(3-(2-acetamidothiazol-4-yl) phenyl)-3,4-dichlorobenzamide (4h), N-(3-(2-acetamidothiazol-4-yl) phenyl)-3-chlorobenzamide (4i) and N-(3-(2-acetamidothiazol-4-yl) phenyl)-2,4-dichlorobenzamide (4o) exhibit moderate antibacterial activity against the tested bacteria.
语种	英语
CSCD记录号	CSCD:6088077
内容类型	期刊论文
源URL	[http://ir.imr.ac.cn/handle/321006/153918]
专题	金属研究所_中国科学院金属研究所
作者单位	1.Jinzhou Med University, Coll Pharm, Jinzhou 121000, Peoples R China 2.辽宁大学 3.中国科学院金属研究所
推荐引用方式 GB/T 7714	Zhang Zhihua,Chen Yu,Chai Baoshan,et al. Synthesis, Anticancer and Antibacterial Activities of Novel 2-Amino-4-phenylthiazole Derivatives Containing Amide Moiety[J]. CHINESE JOURNAL OF ORGANIC CHEMISTRY,2017,37(9):2377-2384.
APA	Zhang Zhihua.,Chen Yu.,Chai Baoshan.,Yang Xiaoman.,Cai Xiaoyu.,...&You Song.(2017).Synthesis, Anticancer and Antibacterial Activities of Novel 2-Amino-4-phenylthiazole Derivatives Containing Amide Moiety.CHINESE JOURNAL OF ORGANIC CHEMISTRY,37(9),2377-2384.
MLA	Zhang Zhihua,et al."Synthesis, Anticancer and Antibacterial Activities of Novel 2-Amino-4-phenylthiazole Derivatives Containing Amide Moiety".CHINESE JOURNAL OF ORGANIC CHEMISTRY 37.9(2017):2377-2384.