Synthesis and biological evaluation of 4,4-dimethyl lithocholic acid derivatives as novel inhibitors of protein tyrosine phosphatase 1B
文献类型：期刊论文
| 作者 | He, Hai-Bing1,3,4; Gao, Li-Xin2; Deng, Qi-Feng3,4; Ma, Wei-Ping2; Tang, Chun-Lan2; Qiu, Wen-Wei3,4; Tang, Jie1,3,4; Li, Jing-Ya2 ; Li, Jia2; Yang, Fan1,3,4
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
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| 出版日期 | 2012-12-01 |
| 卷号 | 22期号:23页码:7237-7242 |
| 关键词 | 4,4-Dimethyl lithocholic acids Protein tyrosine phosphatase 1B Inhibitor SAR Diabetes |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2012.09.040 |
| 文献子类 | Article |
| 英文摘要 | Protein tyrosine phosphatase 1B (PTP1B) is a major negative regulator of both insulin and leptin signals. For years, inhibiting of PTP1B has been considered to be a potential therapeutics for treating Type 2 diabetes and obesity. Recently, we recognized lithocholic acid (LCA) as a natural inhibitor against PTP1B (IC50 = 12.74 mu M) by a vertical screen for the first time. Further SAR research was carried out by synthesizing and evaluating a series of compounds bearing two methyls at C-4 position and a fused heterocycle to ring A. Among them, compound 14b achieved a PTP1B inhibitory activity about eightfold than LCA and a 14-fold selectivity over the homogenous enzyme TCPTP. (C) 2012 Elsevier Ltd. All rights reserved. |
| WOS关键词 | VITAMIN-D-RECEPTOR ; CANCER CELL-LINE ; INSULIN-RECEPTOR ; OLEANOLIC ACID ; PYRAZOLE DERIVATIVES ; SIGNAL-TRANSDUCTION ; HUMAN-PLACENTA ; BILE-ACIDS ; IN-VIVO ; IDENTIFICATION |
| 资助项目 | National Nature Science Foundation of China[81125023] ; National Science and Technology Major Projects for Major New Drugs Innovation and Development[2012ZX09304011] ; Shanghai Science and Technology council[10142200802] ; Shanghai Science and Technology council[11DZ2292200] ; Lab of Organic Functional Molecules, THE SINO-FRENCH INSTITUTE OF ECNU[00000000] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000310583100050 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277869]  |
| 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.E China Normal Univ, Shanghai Engn Res Ctr Mol Theraput & New Drug Dev, Shanghai 200062, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China; 3.E China Normal Univ, Dept Chem, Shanghai 200062, Peoples R China 4.E China Normal Univ, Inst Med Chem, Shanghai 200062, Peoples R China; |
| 推荐引用方式 GB/T 7714 | He, Hai-Bing,Gao, Li-Xin,Deng, Qi-Feng,et al. Synthesis and biological evaluation of 4,4-dimethyl lithocholic acid derivatives as novel inhibitors of protein tyrosine phosphatase 1B[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2012,22(23):7237-7242. |
| APA | He, Hai-Bing.,Gao, Li-Xin.,Deng, Qi-Feng.,Ma, Wei-Ping.,Tang, Chun-Lan.,...&Yang, Fan.(2012).Synthesis and biological evaluation of 4,4-dimethyl lithocholic acid derivatives as novel inhibitors of protein tyrosine phosphatase 1B.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,22(23),7237-7242. |
| MLA | He, Hai-Bing,et al."Synthesis and biological evaluation of 4,4-dimethyl lithocholic acid derivatives as novel inhibitors of protein tyrosine phosphatase 1B".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 22.23(2012):7237-7242. |
入库方式： OAI收割
来源：上海药物研究所
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