Synthesis and biological evaluation of (+/-)-3-(2-(2-fluorobenzyloxy) naphthalen-6-yl)-2-aminopropanoic acid derivatives as novel PTP1B inhibitors
文献类型：期刊论文
| 作者 | Sun, Liang-Peng1; Shen, Qiang2; Piao, Hong-Hua1; Ma, Wei-Ping2; Gao, Li-Xin2; Zhang, Wei2; Nan, Fa-Jun2 ; Li, Jia2; Piao, Hu-Ri1
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| 刊名 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
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| 出版日期 | 2011-09 |
| 卷号 | 46期号:9页码:3630-3638 |
| 关键词 | Protein tyrosine phosphatase 1B Inhibitors 2-Naphthol tyrosine SAR Diabetes |
| ISSN号 | 0223-5234 |
| DOI | 10.1016/j.ejmech.2011.05.027 |
| 文献子类 | Article |
| 英文摘要 | A series of novel nonphosphonate-based pTyr mimetics comprised (+/-)-3-(2-(2-fluorobenzyloxy)naphthalen-6-yl)-2-aminopropanoic acid derivatives were identified as reversible and competitive PTP1B inhibitors via a structure-based design approach. Among the compounds studied, 12h was found to have the best in vitro inhibition activity against PTP1B (IC(50) = 1.25 +/- 0.24 mu M) and the best selectivity (3-fold) between PTP1B and TCPTP. These results should provide suitable druglike lead compounds for the design of inhibitors of PTP1B as well as other PTPs. (C) 2011 Elsevier Masson SAS. All rights reserved. |
| WOS关键词 | TYROSINE-PHOSPHATASE 1B ; INSULIN SIGNAL-TRANSDUCTION ; PROTEIN ; DISCOVERY ; OBESITY ; MICE ; SENSITIVITY ; SPECIFICITY ; RESISTANCE ; ADIPOSITY |
| 资助项目 | National Natural Science Foundation of China[20962021] ; National Science & Technology Major Project of China "Key New Drug Creation and Manufacturing Program"[2009ZX09302-001] ; National Science & Technology Major Project[2007CB914201] ; Natural Science Foundation of China[81021062] ; Natural Science Foundation of China[30801405] ; Shanghai Commission of Science and Technology[09DZ2291200] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000295237400010 |
| 出版者 | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278415]  |
| 专题 | 国家新药筛选中心 药物发现与设计中心 药物安全性评价中心 |
| 通讯作者 | Piao, Hu-Ri |
| 作者单位 | 1.Yanbian Univ, Key Lab Nat Resources Changbai Mt & Funct Mol, Minist Educ, Coll Pharm, Yanji 133000, Peoples R China; 2.Chinese Acad Sci, Natl Ctr Drug Screening, Shanghai Inst Mat Med, Shanghai Inst Biol Sci, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Sun, Liang-Peng,Shen, Qiang,Piao, Hong-Hua,et al. Synthesis and biological evaluation of (+/-)-3-(2-(2-fluorobenzyloxy) naphthalen-6-yl)-2-aminopropanoic acid derivatives as novel PTP1B inhibitors[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2011,46(9):3630-3638. |
| APA | Sun, Liang-Peng.,Shen, Qiang.,Piao, Hong-Hua.,Ma, Wei-Ping.,Gao, Li-Xin.,...&Piao, Hu-Ri.(2011).Synthesis and biological evaluation of (+/-)-3-(2-(2-fluorobenzyloxy) naphthalen-6-yl)-2-aminopropanoic acid derivatives as novel PTP1B inhibitors.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,46(9),3630-3638. |
| MLA | Sun, Liang-Peng,et al."Synthesis and biological evaluation of (+/-)-3-(2-(2-fluorobenzyloxy) naphthalen-6-yl)-2-aminopropanoic acid derivatives as novel PTP1B inhibitors".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 46.9(2011):3630-3638. |
入库方式： OAI收割
来源：上海药物研究所
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