DESIGN, SYNTHESIS AND BIOLOGICAL ACTIVITY EVALUATION OF 2-MERCAPTO-4(3H)-QUINAZOLINONE DERIVATIVES AS NOVEL INHIBITORS OF PROTEIN TYROSINE PHOSPHATASE 1B
文献类型：期刊论文
| 作者 | Li, Hui3; Wang, Jin-Ping3; Yang, Fan3; Liu, Ting3; Qiu, Wen-Wei1; Li, Jing-Ya2 ; Li, Jia2; Tang, Jie3
|
| 刊名 | HETEROCYCLES
 |
| 出版日期 | 2012-08-01 |
| 卷号 | 85期号:8页码:1897-1911 |
| 关键词 | PTP1B TCPTP Quinazolinone Inhibition Synthesis |
| ISSN号 | 0385-5414 |
| DOI | 10.3987/COM-12-12477 |
| 文献子类 | Article |
| 英文摘要 | A series of novel 2-mercapto-4(3H)-quinazolinone derivatives have been synthesized and their inhibitory effects on PTP1B and TCPTP are evaluated for the first time. Most of these derivatives showed good inhibitory activity on PTP1B and reasonable selectivity for PTP1B over TCPTP, among them 32 was the most potent PTP1B inhibitor (IC50 = 1.50 mu g/mL), and 27 possessed the best selectivity of 3.0-fold. |
| WOS关键词 | QUINAZOLINONE DERIVATIVES ; INSULIN SENSITIVITY ; SIGNAL-TRANSDUCTION ; AGENTS ; PTP1B ; DISCOVERY ; RECEPTOR ; OBESITY ; COMPLEX ; POTENT |
| 资助项目 | Shanghai Science and Technology Council[09142200800] ; Shanghai Science and Technology Council[10142200800] ; National Natural Science Foundation of China[20802020] ; Shanghai Key Laboratory of Green Chemistry Processes[00000000] ; Laboratory of Organic Functional Molecules, Sino-French Institute of ECNU[00000000] |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000308897500005 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277991]  |
| 专题 | 国家新药筛选中心 药物安全性评价中心 |
| 通讯作者 | Li, Hui |
| 作者单位 | 1.E China Normal Univ, Dept Chem, Shanghai 200062, Peoples R China; 2.Chinese Acad Sci, Natl Ctr Drug Screening, Shanghai Inst Mat Med, Shanghai Inst Biol Sci, Shanghai 201203, Peoples R China 3.E China Normal Univ, Shanghai Engn Res Ctr Mol Therapeut & New Drug De, Shanghai 200062, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Li, Hui,Wang, Jin-Ping,Yang, Fan,et al. DESIGN, SYNTHESIS AND BIOLOGICAL ACTIVITY EVALUATION OF 2-MERCAPTO-4(3H)-QUINAZOLINONE DERIVATIVES AS NOVEL INHIBITORS OF PROTEIN TYROSINE PHOSPHATASE 1B[J]. HETEROCYCLES,2012,85(8):1897-1911. |
| APA | Li, Hui.,Wang, Jin-Ping.,Yang, Fan.,Liu, Ting.,Qiu, Wen-Wei.,...&Tang, Jie.(2012).DESIGN, SYNTHESIS AND BIOLOGICAL ACTIVITY EVALUATION OF 2-MERCAPTO-4(3H)-QUINAZOLINONE DERIVATIVES AS NOVEL INHIBITORS OF PROTEIN TYROSINE PHOSPHATASE 1B.HETEROCYCLES,85(8),1897-1911. |
| MLA | Li, Hui,et al."DESIGN, SYNTHESIS AND BIOLOGICAL ACTIVITY EVALUATION OF 2-MERCAPTO-4(3H)-QUINAZOLINONE DERIVATIVES AS NOVEL INHIBITORS OF PROTEIN TYROSINE PHOSPHATASE 1B".HETEROCYCLES 85.8(2012):1897-1911. |
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。