Synthesis, Characterization and Biological Activities of 3,5,6-Trisubstituted-1,2,4-triazine Derivatives
文献类型：期刊论文
| 作者 | Li Yingjun1; Shi Xiangling1; Gao Lixin2; Jin Kun3; Sheng Li2; Wu Jianghong1; Peng Lina1; Li Jia2
|
| 刊名 | CHINESE JOURNAL OF ORGANIC CHEMISTRY
 |
| 出版日期 | 2015-01 |
| 卷号 | 35期号:1页码:191-199 |
| 关键词 | 3,5,6-trisubstituted-1,2,4-triazine benzimidazole microwave irradiation synthesis crystal structure Cdc25B and PTP1B inhibitors |
| ISSN号 | 0253-2786 |
| DOI | 10.6023/cjoc201405032 |
| 文献子类 | Article |
| 英文摘要 | Thirty new 3,5,6-trisubstituted-1,2,4-triazine derivatives containing benzimidazole moiety (5 similar to 6) were synthesized via microwave-assisted condensation reactions of 2-aryloxymethylbenzimidazole-1-acetylhydrazines (3) with benzil/p-anisil in the presence of NH4OAc/HOAc. The structures were characterized by elemental analysis, IR, H-1 NMR spectra and single crystal X-ray determination. The synthesized target compounds were evaluated for Cdc25B and PTP1B inhibitory activities. The structure-activity relationship (SAR) was also briefly discussed. The experimental results indicated that some compounds showed good inhibitory activities against Cdc25B and PTP1B. Among of them, compound 6o [IC50 =(0.84 +/- 0.22) mu g/mL.] exhibited highest inhibitory activity against Cdc25B. Compounds 5i, 5m, 5n, 6h, 6j, 6m, 6n and 6o showed higher inhibitory activities against PTP1B [IC50=(0.46 +/- 0.10)similar to(0.87 +/- 0.19) mu g/mL] than positive control oleanolic acid [IC50=(0.97 +/- 0.15) mu g/mL]. It is noteworthy that, compounds 5h, 5m, 6n and 6o showed inhibitory activities against Cdc25B and PTP1B. The target compounds can be considered as potential Cdc25B and PTP1B inhibitors. |
| WOS关键词 | POTENTIAL ANTIMICROBIAL AGENTS ; MICROWAVE-ASSISTED SYNTHESIS ; BENZIMIDAZOLE DERIVATIVES ; ANTITUMOR-ACTIVITY ; INHIBITORS ; COMPLEXES ; CYTOTOXICITY ; SCAFFOLD ; ANALOGS ; DESIGN |
| WOS研究方向 | Chemistry |
| 语种 | 中文 |
| CSCD记录号 | CSCD:5353201 |
| WOS记录号 | WOS:000351191700020 |
| 出版者 | SCIENCE PRESS |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276746]  |
| 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,Shi Xiangling,Gao Lixin,et al. Synthesis, Characterization and Biological Activities of 3,5,6-Trisubstituted-1,2,4-triazine Derivatives[J]. CHINESE JOURNAL OF ORGANIC CHEMISTRY,2015,35(1):191-199. |
| APA | Li Yingjun.,Shi Xiangling.,Gao Lixin.,Jin Kun.,Sheng Li.,...&Li Jia.(2015).Synthesis, Characterization and Biological Activities of 3,5,6-Trisubstituted-1,2,4-triazine Derivatives.CHINESE JOURNAL OF ORGANIC CHEMISTRY,35(1),191-199. |
| MLA | Li Yingjun,et al."Synthesis, Characterization and Biological Activities of 3,5,6-Trisubstituted-1,2,4-triazine Derivatives".CHINESE JOURNAL OF ORGANIC CHEMISTRY 35.1(2015):191-199. |
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。