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![]() |
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:4212-4218 |
关键词 | Click chemistry PTP1B inhibitor Sugar scaffold (Hydroxy)benzoate Molecular docking |
ISSN号 | 0223-5234 |
DOI | 10.1016/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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