SYNTHESIS AND BIOLOGICAL EVALUATION OF OLEANOLIC ACID DERIVATIVES AS NOVEL INHIBITORS OF PROTEIN TYROSINE PHOSPHATASE 1B
文献类型：期刊论文
| 作者 | Li, Hui2; Zou, Hui3; Gao, Lixin1; Liu, Ting2; Yang, Fan2; Lj, Jingya1,3; Li, Jia1 ; Qiu, Wen-Wei3; Tang, Jie2
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| 刊名 | HETEROCYCLES
 |
| 出版日期 | 2012-05-01 |
| 卷号 | 85期号:5页码:1117-1139 |
| 关键词 | PTP1B TCPTP Inhibition |
| ISSN号 | 0385-5414 |
| DOI | 10.3987/COM-12-12445 |
| 文献子类 | Article |
| 英文摘要 | A series of oleanolic acid (OA) derivatives have been synthesized and their inhibitory effects on PTP1B, TCPTP and related PTPs are evaluated. Some compounds with five-membered heterocyclic ring-fused at C-2, C-3 positions showed a dramatic increase in inhibition, the two most potent PTP1B inhibitors 19 (IC50 = 0.91 mu M) and 21 (IC50 = 0.98 mu M) showed about 3-fold more potent than lead compound OA. Some C-ring modified OA analogs showed high selectivity for PTP1B over TCPTP, among them, 50 possessed the best selectivity of 6.6-fold. |
| WOS关键词 | INSULIN-RECEPTOR ; SIGNAL-TRANSDUCTION ; LEPTIN ACTION ; PTP1B ; SENSITIVITY ; ADIPOSITY ; MICE ; TRITERPENOIDS ; DISCOVERY ; GLUCOSE |
| 资助项目 | National Natural Science Foundation of China[20802020] ; Ph.D. Program Foundation of Ministry of Education of China[200802691039] |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000304333500009 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278090]  |
| 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.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, Shanghai Inst Biol Sci, Shanghai 201203, Peoples R China 2.E China Normal Univ, Shanghai Engn Res Ctr Mol Therapeut & New Drug De, Shanghai 200062, Peoples R China; 3.E China Normal Univ, Dept Chem, Shanghai 200062, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Li, Hui,Zou, Hui,Gao, Lixin,et al. SYNTHESIS AND BIOLOGICAL EVALUATION OF OLEANOLIC ACID DERIVATIVES AS NOVEL INHIBITORS OF PROTEIN TYROSINE PHOSPHATASE 1B[J]. HETEROCYCLES,2012,85(5):1117-1139. |
| APA | Li, Hui.,Zou, Hui.,Gao, Lixin.,Liu, Ting.,Yang, Fan.,...&Tang, Jie.(2012).SYNTHESIS AND BIOLOGICAL EVALUATION OF OLEANOLIC ACID DERIVATIVES AS NOVEL INHIBITORS OF PROTEIN TYROSINE PHOSPHATASE 1B.HETEROCYCLES,85(5),1117-1139. |
| MLA | Li, Hui,et al."SYNTHESIS AND BIOLOGICAL EVALUATION OF OLEANOLIC ACID DERIVATIVES AS NOVEL INHIBITORS OF PROTEIN TYROSINE PHOSPHATASE 1B".HETEROCYCLES 85.5(2012):1117-1139. |
入库方式： OAI收割
来源：上海药物研究所
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