Synthesis of triazole-linked beta-C-glycosyl dimers as inhibitors of PTP1B
文献类型：期刊论文
| 作者 | Lin, Li1,2,4; Shen, Qiang3; Chen, Guo-Rong1,4; Xie, Juan2 |
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
 |
| 出版日期 | 2008-11-15 |
| 卷号 | 16期号:22页码:9757-9763 |
| 关键词 | Protein tyrosine phosphatase 1B Diabetes Aryl C-glycosyl compounds Click chemistry 1,4-Benzoquinone 1,4-Naphthoquinone |
| ISSN号 | 0968-0896 |
| DOI | 10.1016/j.bmc.2008.09.066 |
| 文献子类 | Article |
| 英文摘要 | Protein tyrosine phosphatase 1B (PTP1B) has emerged as a promising target for type 2 diabetes. We have successfully synthesized dimeric acetylated and benzoylated beta-C-D-glucosyl and beta-C-D-galactosyl 1,4-dimethoxy benzenes or naphthalenes by click chemistry. These compounds were further transformed into the corresponding beta-C-D-glycosyl-1,4-quinone derivatives by CAN oxidation. The in vitro inhibition test showed that dimeric benzoylated beta-C-D-glycosyl 1,4-dimethoxybenzenes or 1,4-benzoquinones were good inhibitors of PTP1B (IC50: 0.62-0.88 mu M), with no significant difference between gluco and galacto derivatives. (C) 2008 Elsevier Ltd. All rights reserved. |
| WOS关键词 | PROTEIN-TYROSINE PHOSPHATASES ; INSULIN SIGNAL-TRANSDUCTION ; CLICK CHEMISTRY ; ALLOSTERIC INHIBITION ; ACID ; 1B ; IDENTIFICATION ; SENSITIVITY ; DERIVATIVES ; GENERATION |
| 资助项目 | CNRS[00000000] ; ENS Cachan[00000000] ; National Natural Science Foundation of China[20876045] ; Shanghai Science and Technology Community[074107018] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000260758200014 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279433]  |
| 专题 | 国家新药筛选中心 |
| 通讯作者 | Chen, Guo-Rong |
| 作者单位 | 1.E China Univ Sci & Technol, Inst Fine Chem, Shanghai 200237, Peoples R China; 2.ENS, CNRS, UniverSud, PPSM, F-94230 Cachan, France; 3.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China 4.E China Univ Sci & Technol, Adv Mat Lab, Shanghai 200237, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Lin, Li,Shen, Qiang,Chen, Guo-Rong,et al. Synthesis of triazole-linked beta-C-glycosyl dimers as inhibitors of PTP1B[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2008,16(22):9757-9763. |
| APA | Lin, Li,Shen, Qiang,Chen, Guo-Rong,&Xie, Juan.(2008).Synthesis of triazole-linked beta-C-glycosyl dimers as inhibitors of PTP1B.BIOORGANIC & MEDICINAL CHEMISTRY,16(22),9757-9763. |
| MLA | Lin, Li,et al."Synthesis of triazole-linked beta-C-glycosyl dimers as inhibitors of PTP1B".BIOORGANIC & MEDICINAL CHEMISTRY 16.22(2008):9757-9763. |
入库方式： OAI收割
来源：上海药物研究所
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