1H-2,3-Dihydroperimidine Derivatives: A New Class of Potent Protein Tyrosine Phosphatase 1B Inhibitors
文献类型：期刊论文
| 作者 | Wang, Wen-Long1,2,3; Yang, Dong-Lin2; Gao, Li-Xin1; Tang, Chun-Lan1; Ma, Wei-Ping1; Ye, Hui-Hua2; Zhang, Si-Qi2; Zhao, Ya-Nan2; Xu, Hao-Jie2; Hu, Zhao2 |
| 刊名 | MOLECULES
 |
| 出版日期 | 2014-01 |
| 卷号 | 19期号:1页码:102-121 |
| 关键词 | 1H-2,3-dihydroperimidine derivatives PTP1B inhibitors selectivity structure-activity relationships (SAR) |
| ISSN号 | 1420-3049 |
| DOI | 10.3390/molecules19010102 |
| 文献子类 | Article |
| 英文摘要 | A series of 1H-2,3-dihydroperimidine derivatives was designed, synthesized, and evaluated as a new class of inhibitors of protein tyrosine phosphatase 1B (PTP1B) with IC50 values in the micromolar range. Compounds 46 and 49 showed submicromolar inhibitory activity against PTP1B, and good selectivity (3.48-fold and 2.10-fold respectively) over T-cell protein tyrosine phosphatases (TCPTP). These results have provided novel lead compounds for the design of inhibitors of PTP1B as well as other PTPs. |
| WOS关键词 | MOLECULE KINASE INHIBITORS ; INSULIN SENSITIVITY ; DRUG TARGETS ; CANCER ; PTP1B ; MICE ; DISCOVERY ; MECHANISM |
| 资助项目 | National Natural Science Foundation of China[81125023] ; State Key Laboratory of Drug Research[SIMM1302KF-05] ; Fundamental Research Funds for the Central Universities[JUSRP1040] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000334420300007 |
| 出版者 | MDPI AG |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277293]  |
| 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 |
| 通讯作者 | Wang, Wen-Long |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, State key Lab Drug Res, Shanghai 201203, Peoples R China; 2.Jiangnan Univ, Sch Pharmaceut Sci, Wuxi 214122, Peoples R China; 3.Jiangshu Alpha Biopharmaceut Inc, Wuxi 214122, Peoples R China |
| 推荐引用方式 GB/T 7714 | Wang, Wen-Long,Yang, Dong-Lin,Gao, Li-Xin,et al. 1H-2,3-Dihydroperimidine Derivatives: A New Class of Potent Protein Tyrosine Phosphatase 1B Inhibitors[J]. MOLECULES,2014,19(1):102-121. |
| APA | Wang, Wen-Long.,Yang, Dong-Lin.,Gao, Li-Xin.,Tang, Chun-Lan.,Ma, Wei-Ping.,...&Feng, Bainian.(2014).1H-2,3-Dihydroperimidine Derivatives: A New Class of Potent Protein Tyrosine Phosphatase 1B Inhibitors.MOLECULES,19(1),102-121. |
| MLA | Wang, Wen-Long,et al."1H-2,3-Dihydroperimidine Derivatives: A New Class of Potent Protein Tyrosine Phosphatase 1B Inhibitors".MOLECULES 19.1(2014):102-121. |
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。