Synthesis, Anticancer and Antibacterial Activities of Novel 2-Amino-4-phenylthiazole Derivatives Containing Amide Moiety
文献类型：期刊论文
| 作者 | Zhang Zhihua3; Chen Yu3; Chai Baoshan3; Yang Xiaoman1; Cai Xiaoyu1; Cui Bo1; You Song3 |
| 刊名 | CHINESE JOURNAL OF ORGANIC CHEMISTRY
 |
| 出版日期 | 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 |
| 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. |
入库方式： OAI收割
来源：金属研究所
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