Microwave-Assisted Synthesis and Biological Activities of 3,6-Disubstituted-1,2,4-triazine Derivatives
文献类型：期刊论文
| 作者 | Li Yingjun1; Shao Xin1; Gao Lixin2; Jin Kun3; Sheng Li2; Luo Tongchuan1; Yu Yang1; Li Jia2
|
| 刊名 | CHINESE JOURNAL OF ORGANIC CHEMISTRY
 |
| 出版日期 | 2013-10 |
| 卷号 | 33期号:10页码:2178-2185 |
| 关键词 | microwave irradiation 1,2,4-triazines benzimidazole synthesis Cdc25B and PTP1B inhibitors |
| ISSN号 | 0253-2786 |
| DOI | 10.6023/cjoc201304011 |
| 文献子类 | Article |
| 英文摘要 | Twenty new 3,6-disubstituted-1,2,4-triazine derivatives containing benzimidazole moiety (4) were synthesized via microwave-assisted condensation reactions of 2-aryloxymethylbenzimidazole-1-acetylhydrazines (3) with various (un)substituted phenacyl bromides in DMF. The structures were characterized by IR, H-1 NMR spectra and elemental analysis. The optimum experimental conditions were found. Compared with traditional methods, this synthetic method has such advantages as short reaction time, simple operation, broad substrate scope, easy purification and high yields. The synthesized target compounds were screened for Cdc25B and PTP1B inhibitory activities. The experimental results indicate that compounds 4g and 4j showed good inhibitory activities against Cdc25B, and 4a, 4h, 4j, 4r and 4s exhibited potent inhibitory activities against PTP1B. It is noteworthy that compound 4j can be used as potential Cdc25B and PTP1B inhibitors in the treatment of cancer and diabetes. |
| WOS关键词 | ONE-POT SYNTHESIS ; BENZIMIDAZOLE DERIVATIVES ; 1,2,4-TRIAZINES ; AGENTS ; INHIBITORS ; PTP1B |
| 资助项目 | Natural Science Foundation of Liaoning Province[20102126] |
| WOS研究方向 | Chemistry |
| 语种 | 中文 |
| CSCD记录号 | CSCD:4973047 |
| WOS记录号 | WOS:000327365900014 |
| 出版者 | SCIENCE PRESS |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277431]  |
| 专题 | 国家新药筛选中心 中科院受体结构与功能重点实验室 新药研究国家重点实验室 药物安全性评价中心 |
| 通讯作者 | Li Yingjun |
| 作者单位 | 1.Liaoning Normal Univ, Coll Chem & Chem Engn, Dalian 116029, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 3.Dalian Univ Technol, State Key Lab Fine Chem, Dalian 116012, Peoples R China |
| 推荐引用方式 GB/T 7714 | Li Yingjun,Shao Xin,Gao Lixin,et al. Microwave-Assisted Synthesis and Biological Activities of 3,6-Disubstituted-1,2,4-triazine Derivatives[J]. CHINESE JOURNAL OF ORGANIC CHEMISTRY,2013,33(10):2178-2185. |
| APA | Li Yingjun.,Shao Xin.,Gao Lixin.,Jin Kun.,Sheng Li.,...&Li Jia.(2013).Microwave-Assisted Synthesis and Biological Activities of 3,6-Disubstituted-1,2,4-triazine Derivatives.CHINESE JOURNAL OF ORGANIC CHEMISTRY,33(10),2178-2185. |
| MLA | Li Yingjun,et al."Microwave-Assisted Synthesis and Biological Activities of 3,6-Disubstituted-1,2,4-triazine Derivatives".CHINESE JOURNAL OF ORGANIC CHEMISTRY 33.10(2013):2178-2185. |
入库方式： OAI收割
来源：上海药物研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。