Synthesis and Cell Division Cycle 25B Phosphatase and Protein Tyrosine Phosphatase 1B Inhibitory Activity Evaluation of Novel 3,6-Disubstituted Triazolothiadiazole Derivatives
文献类型：期刊论文
| 作者 | Li Yingjun1; Li Jiyang1; Peng Lina1; Gao Lixin3; Jin Kun2; Sheng Li3; Zhang Nan1; Wang Siyuan1; Li Jia3
|
| 刊名 | CHINESE JOURNAL OF ORGANIC CHEMISTRY
 |
| 出版日期 | 2017-02-25 |
| 卷号 | 37期号:2页码:485-495 |
| 关键词 | triazolothiadiazole benzimidazole arylsulfonyl synthesis Cdc25B and PTP1B inhibitors |
| ISSN号 | 0253-2786 |
| DOI | 10.6023/cjoc201607030 |
| 文献子类 | Article |
| 英文摘要 | A series of new 3,6-disubstituted triazolothiadiazole derivatives 7a similar to 7y containing benzimidazole and arylsulfonyl moities have been synthesized by o-pheny lenediamine and chloroacetic acid as starting materials via multistep reactions. The structures of the intermediates 3, 4, 6 and the target compounds 7 were characterized by H-1 NMR, IR spectra and elemental analysis. All synthesized target compounds were screened for their inhibitory activity against cell division cycle 25B phosphatase (Cdc25B) and protein tyrosine phosphatase 1B (PTP1B). The results show that some of them display significant inhibitory activities against Cdc25B and PTP1B. Among them, compound 7d exhibits the highest inhibitory activity against Cdc25B [ IC50=(7.72 perpendicular to 0.73) mu g/mL] and 7u exhibits the highest inhibitory activity against PTP1B [ IC50=(3.31 perpendicular to 0.57) mu g/mL]. It is noteworthy that compounds 7b, 7d, 7l, 7t and 7u show higher inhibitory activities against Cdc25B and PTP1B. They can be considered as potential Cdc25B and PTP1B inhibitors, and have great application prospects in the treatment of cancers and diabetes. |
| WOS关键词 | BIOLOGICAL-ACTIVITIES ; ANTICANCER AGENTS ; PTP1B INHIBITORS ; SCAFFOLDS ; ANALOGS ; DESIGN ; MOIETY ; ACID |
| 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:5947952 |
| WOS记录号 | WOS:000397808100022 |
| 出版者 | SCIENCE PRESS |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/272767]  |
| 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; Li Jia |
| 作者单位 | 1.Liaoning Normal Univ, Coll Chem & Chem Engn, Dalian 116029, Peoples R China; 2.Dalian Univ Technol, State Key Lab Fine Chem, Dalian 116012, Peoples R China 3.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, State Key Lab Drug Res, Shanghai 201203, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Li Yingjun,Li Jiyang,Peng Lina,et al. Synthesis and Cell Division Cycle 25B Phosphatase and Protein Tyrosine Phosphatase 1B Inhibitory Activity Evaluation of Novel 3,6-Disubstituted Triazolothiadiazole Derivatives[J]. CHINESE JOURNAL OF ORGANIC CHEMISTRY,2017,37(2):485-495. |
| APA | Li Yingjun.,Li Jiyang.,Peng Lina.,Gao Lixin.,Jin Kun.,...&Li Jia.(2017).Synthesis and Cell Division Cycle 25B Phosphatase and Protein Tyrosine Phosphatase 1B Inhibitory Activity Evaluation of Novel 3,6-Disubstituted Triazolothiadiazole Derivatives.CHINESE JOURNAL OF ORGANIC CHEMISTRY,37(2),485-495. |
| MLA | Li Yingjun,et al."Synthesis and Cell Division Cycle 25B Phosphatase and Protein Tyrosine Phosphatase 1B Inhibitory Activity Evaluation of Novel 3,6-Disubstituted Triazolothiadiazole Derivatives".CHINESE JOURNAL OF ORGANIC CHEMISTRY 37.2(2017):485-495. |
入库方式： OAI收割
来源：上海药物研究所
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