Synthesis and Biological Evaluation of 2,4,6-Trihydroxychalcone Derivatives as Novel Protein Tyrosine Phosphatase 1B Inhibitors
文献类型：期刊论文
| 作者 | Sun, Liang-Peng2; Gao, Li-Xin1; Ma, Wei-Ping1; Nan, Fa-Jun1 ; Li, Jia1; Piao, Hu-Ri2
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| 刊名 | CHEMICAL BIOLOGY & DRUG DESIGN
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| 出版日期 | 2012-10 |
| 卷号 | 80期号:4页码:584-590 |
| 关键词 | 2 4 6-trihydroxychalcone diabetes inhibitors protein tyrosine phosphatase 1B structure-activity relationship |
| ISSN号 | 1747-0277 |
| DOI | 10.1111/j.1747-0285.2012.01431.x |
| 文献子类 | Article |
| 英文摘要 | A series of 2,4,6-trihydroxychalcone derivatives were synthesized and identified as reversible and competitive protein tyrosine phosphatase (PTP) 1B inhibitors with IC50 values in the micromolar range. Compound 4a had the greatest in vitro inhibition activity against PTP1B (IC50 = 0.27 +/- 0.01 mu m) and the best selectivity (6.9-fold) for PTP1B relative to T-cell protein tyrosine phosphatases. The compounds identified herein provide a foundation on which to design specific inhibitors of PTP1B and other PTPs. |
| WOS关键词 | INSULIN SENSITIVITY ; ANTIOXIDATIVE ACTIVITY ; PRENYLATED CHALCONES ; SIGNAL-TRANSDUCTION ; OBESITY ; CANCER ; PTP1B ; MICE ; FLAVONOIDS ; RECEPTOR |
| 资助项目 | National Natural Science Foundation of China[20962021] ; National Natural Science Foundation of China[81125023] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000308994500010 |
| 出版者 | WILEY |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277923]  |
| 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 | Li, Jia |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Biol Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening,State Key Lab Drug Res, Shanghai 201203, Peoples R China; 2.Yanbian Univ, Coll Pharm, Key Lab Nat Resources Changbai Mt & Funct Mol, Yanji 133000, Peoples R China |
| 推荐引用方式 GB/T 7714 | Sun, Liang-Peng,Gao, Li-Xin,Ma, Wei-Ping,et al. Synthesis and Biological Evaluation of 2,4,6-Trihydroxychalcone Derivatives as Novel Protein Tyrosine Phosphatase 1B Inhibitors[J]. CHEMICAL BIOLOGY & DRUG DESIGN,2012,80(4):584-590. |
| APA | Sun, Liang-Peng,Gao, Li-Xin,Ma, Wei-Ping,Nan, Fa-Jun,Li, Jia,&Piao, Hu-Ri.(2012).Synthesis and Biological Evaluation of 2,4,6-Trihydroxychalcone Derivatives as Novel Protein Tyrosine Phosphatase 1B Inhibitors.CHEMICAL BIOLOGY & DRUG DESIGN,80(4),584-590. |
| MLA | Sun, Liang-Peng,et al."Synthesis and Biological Evaluation of 2,4,6-Trihydroxychalcone Derivatives as Novel Protein Tyrosine Phosphatase 1B Inhibitors".CHEMICAL BIOLOGY & DRUG DESIGN 80.4(2012):584-590. |
入库方式： OAI收割
来源：上海药物研究所
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