Discovery of core-structurally novel PTP1B inhibitors with specific selectivity containing oxindole-fused spirotetrahydrofurochroman by one-pot reaction
文献类型：期刊论文
| 作者 | Dong, Suzhen1; Lei, Yubing1; Jia, Shikun1; Gao, Lixin2; Li, Jia2 ; Zhu, Tong1; Liu, Shunying1; Hu, Wenhao1
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
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| 出版日期 | 2017-02-15 |
| 卷号 | 27期号:4页码:1105-1108 |
| 关键词 | PTP1B inhibitor New structure Oxindole Polycycle Spirotetrahydrofurochroman |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2016.11.055 |
| 文献子类 | Article |
| 英文摘要 | Protein tyrosine phosphatase 1B (PTP1B) has been proposed to be an ideal target for treatment of type II diabetes and obesity. However, no druggable PTP1B inhibitor has been established and there is still an urgent demand for the development of structurally novel PTPIB inhibitor. Herein, we reported core-structurally novel PTP1B inhibitors with low micromole-ranged inhibitory activity by one-pot reaction from simple starting materials. Further studies demonstrated some of these active compounds had a specific selectivity over other PTPs. The structure and activity relationship was also described. The best active and selective compound 5e inhibited PTP1B activity with an IC50 of 4.53 mu M. Molecular docking analysis further demonstrated that compound 5e bound to the active pocket of PTP1B. The results might provide some insights for further development of new drugs for type II diabetes and obesity. (C) 2016 Elsevier Ltd. All rights reserved. |
| WOS关键词 | TYROSINE-PHOSPHATASE 1B ; INSULIN SENSITIVITY ; CASCADE REACTIONS ; PROTEIN ; MICE ; GLUCOSE ; OBESITY ; DESIGN ; ACID |
| 资助项目 | National Natural Science Foundation of China[21332003] ; National Natural Science Foundation of China[21672066] ; Natural Science Foundation of Shanghai[15ZR1411000] ; Natural Science Foundation of Shanghai[16ZR1410500] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000395967700074 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/275628]  |
| 专题 | 国家新药筛选中心 中科院受体结构与功能重点实验室 新药研究国家重点实验室 药物安全性评价中心 |
| 通讯作者 | Liu, Shunying; Hu, Wenhao |
| 作者单位 | 1.East China Normal Univ, Shanghai Engn Res Ctr Mol Therapeut & New Drug De, Sch Chem & Mol Engn, 3663 North Zhongshan Rd, Shanghai 200062, Peoples R China; 2.Chinese Acad Sci, Natl Ctr Drug Screening, State Key Lab Drug Res, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Dong, Suzhen,Lei, Yubing,Jia, Shikun,et al. Discovery of core-structurally novel PTP1B inhibitors with specific selectivity containing oxindole-fused spirotetrahydrofurochroman by one-pot reaction[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2017,27(4):1105-1108. |
| APA | Dong, Suzhen.,Lei, Yubing.,Jia, Shikun.,Gao, Lixin.,Li, Jia.,...&Hu, Wenhao.(2017).Discovery of core-structurally novel PTP1B inhibitors with specific selectivity containing oxindole-fused spirotetrahydrofurochroman by one-pot reaction.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,27(4),1105-1108. |
| MLA | Dong, Suzhen,et al."Discovery of core-structurally novel PTP1B inhibitors with specific selectivity containing oxindole-fused spirotetrahydrofurochroman by one-pot reaction".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 27.4(2017):1105-1108. |
入库方式： OAI收割
来源：上海药物研究所
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