Synthesis and Biological Evaluation of Heterocyclic Ring-substituted Chalcone Derivatives as Novel Inhibitors of Protein Tyrosine Phosphatase 1B | |
Chen, Zhen-Hua1; Sun, Liang-Peng1; Zhang, Wei2; Shen, Qiang2; Gao, Li-Xin2; Li, Jia2![]() | |
刊名 | BULLETIN OF THE KOREAN CHEMICAL SOCIETY
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2012-05-20 | |
卷号 | 33期号:5页码:1505-1508 |
关键词 | Chalcone Protein tyrosine phosphatase 1B Inhibitor SAR |
ISSN号 | 0253-2964 |
DOI | 10.5012/bkcs.2012.33.5.1505 |
文献子类 | Article |
英文摘要 | Protein tyrosine phosphatase 1B (PTP1B) is a key factor in negative regulation of the insulin pathway, and is a promising target for the treatment of type-II diabetes, obesity and cancer. Herein, compound (4) was first observed to have moderate inhibitory activity against PTP1B with an IC50 value of 13.72 +/- 1.53 mu M. To obtain more potent PTP1B inhibitors, we synthesized a series of chalcone derivatives using compound (4) as the lead compound. Compound 4I (IC50 = 3.12 +/- 0.18 mu M) was 4.4-fold more potent than the lead compound 4 (IC50 = 13.72 +/- 1.53 mu M), and more potent than the positive control, ursolic acid (IC50=3.40 +/- 0.21 mu M). These results may help to provide suitable drug-like lead compounds for the design of inhibitors of PTP1B as well as other PTPs. |
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关键词 | INSULIN-RECEPTOR ; SIGNAL-TRANSDUCTION ; DISCOVERY ; OBESITY ; SENSITIVITY ; CANCER ; SERIES ; PTP1B ; ACID ; MICE |
WOS研究方向 | Chemistry |
语种 | 英语 |
出版者 | KOREAN CHEMICAL SOC |
WOS记录号 | WOS:000304432100013 |
内容类型 | 期刊论文 |
源URL | [http://119.78.100.183/handle/2S10ELR8/278074] ![]() |
专题 | 国家新药筛选中心 药物安全性评价中心 |
通讯作者 | Li, Jia |
作者单位 | 1.Yanbian Univ, Coll Pharm, Key Lab Nat Resources & Funct Mol Changbai Mt, Affiliated Minist Educ, Yanji 133002, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai Inst Biol Sci, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China; |
推荐引用方式 GB/T 7714 | Chen, Zhen-Hua,Sun, Liang-Peng,Zhang, Wei,et al. Synthesis and Biological Evaluation of Heterocyclic Ring-substituted Chalcone Derivatives as Novel Inhibitors of Protein Tyrosine Phosphatase 1B[J]. BULLETIN OF THE KOREAN CHEMICAL SOCIETY,2012,33(5):1505-1508. |
APA | Chen, Zhen-Hua.,Sun, Liang-Peng.,Zhang, Wei.,Shen, Qiang.,Gao, Li-Xin.,...&Piao, Hu-Ri.(2012).Synthesis and Biological Evaluation of Heterocyclic Ring-substituted Chalcone Derivatives as Novel Inhibitors of Protein Tyrosine Phosphatase 1B.BULLETIN OF THE KOREAN CHEMICAL SOCIETY,33(5),1505-1508. |
MLA | Chen, Zhen-Hua,et al."Synthesis and Biological Evaluation of Heterocyclic Ring-substituted Chalcone Derivatives as Novel Inhibitors of Protein Tyrosine Phosphatase 1B".BULLETIN OF THE KOREAN CHEMICAL SOCIETY 33.5(2012):1505-1508. |
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