中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
Click to a focused library of benzyl 6-triazolo(hydroxy)benzoic glucosides: Novel construction of PTP1B inhibitors on a sugar scaffold

文献类型:期刊论文

作者Li, Cui1,2; He, Xiao-Peng1,2,4; Zhang, Yin-Jie1,2; Li, Zhen1,2; Gao, Li-Xin3; Shi, Xiao-Xin1,2; Xie, Juan4; Li, Jia3; Chen, Guo-Rong1,2; Tang, Yun1,2
刊名EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
出版日期2011-09
卷号46期号:9页码:4212-4218
关键词Click chemistry PTP1B inhibitor Sugar scaffold (Hydroxy)benzoate Molecular docking
ISSN号0223-5234
DOI10.1016/j.ejmech.2011.06.025
文献子类Article
英文摘要With an aim of developing novel protein tyrosine phosphatase (PTP) 1B inhibitors based on sugar scaffolds, a focused library of benzyl 6-triazolo(hydroxy)benzoic glucosides was efficiently constructed via the modular and selective Cu(l)-catalyzed azide-alkyne 1,3-dipolar cycloaddtion (click chemistry). These glycoconjugates bearing alkyl chain length-varied bridges between the sugar and (hydroxy)benzoic moieties were identified as new PTP1B inhibitors with selectivity over T-Cell PTP (TCPTP), SH2-Containing PTP-1 (SHP-1), SHP-2 and Leukocyte Antigen-Related Tyrosine Phosphatase (LAR). Molecular docking study sequentially elaborated the plausible binding modes of the structurally diverse sugar-based inhibitors with PTP1B. (C) 2011 Elsevier Masson SAS. All rights reserved.
WOS关键词TYROSINE-PHOSPHATASE 1B ; COMPETITIVE INHIBITOR ; DISCOVERY ; CHEMISTRY ; DRUG ; DERIVATIVES ; ACIDS
资助项目National Natural Science Foundation of China[20876045] ; National Natural Science Foundation of China[30801405] ; National Basic Research Program of China[2007CB914201] ; Shanghai Science and Technology Community[10410702700] ; Shanghai Science and Technology Community[KSCX2-EW-R-15] ; Fundamental Research Funds for the Central Universities[WK1013002] ; French Embassy in Beijing, China[00000000]
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000295237400071
出版者ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
源URL[http://119.78.100.183/handle/2S10ELR8/278416]  
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Chen, Guo-Rong
作者单位1.E China Univ Sci & Technol, Sch Pharm, Shanghai 200237, Peoples R China;
2.E China Univ Sci & Technol, Key Lab Adv Mat & Fine Chem, Shanghai 200237, Peoples R China;
3.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China;
4.CNRS, UMR 8531, PPSM, Inst Alembert,ENS Cachan, F-94235 Cachan, France
推荐引用方式
GB/T 7714
Li, Cui,He, Xiao-Peng,Zhang, Yin-Jie,et al. Click to a focused library of benzyl 6-triazolo(hydroxy)benzoic glucosides: Novel construction of PTP1B inhibitors on a sugar scaffold[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2011,46(9):4212-4218.
APA Li, Cui.,He, Xiao-Peng.,Zhang, Yin-Jie.,Li, Zhen.,Gao, Li-Xin.,...&Tang, Yun.(2011).Click to a focused library of benzyl 6-triazolo(hydroxy)benzoic glucosides: Novel construction of PTP1B inhibitors on a sugar scaffold.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,46(9),4212-4218.
MLA Li, Cui,et al."Click to a focused library of benzyl 6-triazolo(hydroxy)benzoic glucosides: Novel construction of PTP1B inhibitors on a sugar scaffold".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 46.9(2011):4212-4218.

入库方式: OAI收割

来源:上海药物研究所

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