Synthesis and biological evaluation of novel bis-aromatic amides as novel PTP1B inhibitors
文献类型：期刊论文
| 作者 | Wang, Wen-Long1,2; Huang, Chao1; Gao, Li-Xin2; Tang, Chun-Lan2; Wang, Jun-Qing1; Wu, Min-Chen1; Sheng, Li2; Chen, Hai-Jun2; Nan, Fa-Jun2 ; Li, Jing-Ya2
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
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| 出版日期 | 2014-04-15 |
| 卷号 | 24期号:8页码:1889-1894 |
| 关键词 | Bis-aromatic amides PTP1B inhibitors Selectivity Cellular activity Structure-activity relationships (SARs) |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2014.03.015 |
| 文献子类 | Article |
| 英文摘要 | A series of bis-aromatic amides was designed, synthesized, and evaluated as a new class of inhibitors with IC50 values in the micromolar range against protein tyrosine phosphatase 1B (PTP1B). Among them, compound 15 displayed an IC50 value of 2.34 +/- 0.08 mu M with 5-fold preference over TCPTP. More importantly, the treatment of CHO/HIR cells with compound 15 resulted in increased phosphorylation of insulin receptor (IR), which suggested extensive cellular activity of compound 15. These results provided novel lead compounds for the design of inhibitors of PTP1B as well as other PTPs. (C) 2014 Elsevier Ltd. All rights reserved. |
| WOS关键词 | PROTEIN-TYROSINE PHOSPHATASES ; MOLECULE KINASE INHIBITORS ; DRUG TARGETS ; CANCER ; DISCOVERY ; MECHANISM ; POTENT ; 1B |
| 资助项目 | National Natural Science Foundation of China[81125023] ; State Key Laboratory of Drug Research[SIMM1302KF-05] ; Fundamental Research Funds for the Central Universities[JUSRP1040] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000333579500005 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277114]  |
| 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 |
| 通讯作者 | Wang, Wen-Long |
| 作者单位 | 1.Jiangnan Univ, Sch Pharmaceut Sci, Wuxi 214122, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 3.Jiangsu Alpha Biopharmaceut Inc, Wuxi 214122, Peoples R China |
| 推荐引用方式 GB/T 7714 | Wang, Wen-Long,Huang, Chao,Gao, Li-Xin,et al. Synthesis and biological evaluation of novel bis-aromatic amides as novel PTP1B inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2014,24(8):1889-1894. |
| APA | Wang, Wen-Long.,Huang, Chao.,Gao, Li-Xin.,Tang, Chun-Lan.,Wang, Jun-Qing.,...&Feng, Bainian.(2014).Synthesis and biological evaluation of novel bis-aromatic amides as novel PTP1B inhibitors.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,24(8),1889-1894. |
| MLA | Wang, Wen-Long,et al."Synthesis and biological evaluation of novel bis-aromatic amides as novel PTP1B inhibitors".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 24.8(2014):1889-1894. |
入库方式： OAI收割
来源：上海药物研究所
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