Synthesis and biological evaluation of heterocyclic ring-substituted maslinic acid derivatives as novel inhibitors of protein tyrosine phosphatase 1B
文献类型：期刊论文
| 作者 | Qiu, Wen-Wei2; Shen, Qiang1; Yang, Fan2; Wang, Bo2; Zou, Hui2; Li, Jing-Ya1 ; Li, Jia1; Tang, Jie2
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2009-12-01 |
| 卷号 | 19期号:23页码:6618-6622 |
| 关键词 | Maslinic acid Protein tyrosine phosphatase 1B Inhibitor SAR Diabetes |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2009.10.017 |
| 文献子类 | Article |
| 英文摘要 | A series of maslinic acid derivatives have been synthesized by introducing various fused heterocyclic rings at C-2 and C-3 positions. Their inhibitory effects on PTP1B, TCPTP and related PTPs are evaluated. Most of the compounds exhibited a dramatic increase in inhibitory potency and selectivity, the two most potent PTP1B inhibitors 20 (IC50 = 0.61 mu M) and 29 (IC50 = 0.64 mu M) showed about 10-fold more potent than lead compound maslinic acid. More importantly, 29 possesses the best selectivity of 6.9-fold for PTP1B over TCPTP. (C) 2009 Elsevier Ltd. All rights reserved. |
| WOS关键词 | OCCURRING PENTACYCLIC TRITERPENES ; SIDE-CHAIN MIMETICS ; COLON-CANCER CELLS ; INSULIN-RECEPTOR ; SIGNAL-TRANSDUCTION ; GLYCOGEN-PHOSPHORYLASE ; NATURAL-PRODUCTS ; APOPTOSIS ; MICE ; MACROPHAGES |
| 资助项目 | National Natural Science Foundation of China[20802020] ; Ministry of Education of China[200802691039] ; Shanghai Science and Technology Council[8QH14005] ; Shanghai Science and Technology Council[09JC1404900] ; Hi- Tech Research and Development Program of China[2006AA02Z315] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000271430400027 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279069]  |
| 专题 | 国家新药筛选中心 药物安全性评价中心 |
| 通讯作者 | Li, Jia |
| 作者单位 | 1.Chinese Acad Sci, Natl Ctr Drug Screening, Shanghai Inst Mat Med, Shanghai Inst Biol Sci, Shanghai 201203, Peoples R China; 2.E China Normal Univ, Inst Med Chem, Dept Chem, Shanghai 200062, Peoples R China |
| 推荐引用方式 GB/T 7714 | Qiu, Wen-Wei,Shen, Qiang,Yang, Fan,et al. Synthesis and biological evaluation of heterocyclic ring-substituted maslinic acid derivatives as novel inhibitors of protein tyrosine phosphatase 1B[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2009,19(23):6618-6622. |
| APA | Qiu, Wen-Wei.,Shen, Qiang.,Yang, Fan.,Wang, Bo.,Zou, Hui.,...&Tang, Jie.(2009).Synthesis and biological evaluation of heterocyclic ring-substituted maslinic acid derivatives as novel inhibitors of protein tyrosine phosphatase 1B.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,19(23),6618-6622. |
| MLA | Qiu, Wen-Wei,et al."Synthesis and biological evaluation of heterocyclic ring-substituted maslinic acid derivatives as novel inhibitors of protein tyrosine phosphatase 1B".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 19.23(2009):6618-6622. |
入库方式： OAI收割
来源：上海药物研究所
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