Synthesis and Protein Tyrosine Phosphatase 1B Inhibitory Activity of Novel Chalcone Derivatives Containing 3,4-Dihydroquinolin-2(1H)-one Moiety
文献类型：期刊论文
| 作者 | Sun Liangpeng3; Jiang Zhe1; Gao Lixin2; Li Yingzhe3; Sun Liyun3; Li Jia2 ; Piao, Huri3
|
| 刊名 | CHINESE JOURNAL OF ORGANIC CHEMISTRY
 |
| 出版日期 | 2012-11 |
| 卷号 | 32期号:11页码:2108-2114 |
| 关键词 | chalcone 3,4-dihydroquinolin-2(1H)-one PTP1B inhibitor |
| ISSN号 | 0253-2786 |
| DOI | 10.6023/cjoc201206018 |
| 文献子类 | Article |
| 英文摘要 | Protein tyrosine phosphatase 1B (PTP1B) has recently been identified as new drug target for type II diabetes and obesity due to it is a negative regulator of the insulin and leptin-signaling pathway. In order to find new nonphosphonate-based pTyr mimetics, a series of novel chalcone derivatives bearing the 3,4-dihydroquinolin-2(1H)-one moieties (4a similar to 4n) were designed, synthesized, and evaluated for their PTP1B inhibitory activity. The results demonstrated that all compounds presented potent inhibitory activities against PTP1B, among which compounds 4e and 4i exhibited most potent with IC50 value of (4.64 +/- 0.38) and (4.36 +/- 0.41) mu mol/L, respectively. |
| WOS关键词 | INSULIN SENSITIVITY ; ANTIOXIDATIVE ACTIVITY ; PRENYLATED CHALCONES ; OBESITY ; PTP1B ; ACID ; MICE ; CYTOTOXICITY ; DISCOVERY ; ADIPOSITY |
| 资助项目 | National Natural Science Foundation of China[20962021] ; National Natural Science Foundation of China[81125023] |
| WOS研究方向 | Chemistry |
| 语种 | 中文 |
| CSCD记录号 | CSCD:4719225 |
| WOS记录号 | WOS:000312684100011 |
| 出版者 | SCIENCE PRESS |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277877]  |
| 专题 | 国家新药筛选中心 药物安全性评价中心 |
| 通讯作者 | Sun Liyun |
| 作者单位 | 1.Yanbian Univ Hosp, Yanji 133002, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China 3.Yanbian Univ, Coll Pharm, Minist Educ, Key Lab Nat Resources Changbai Mt & Funct Mol, Yanji 133002, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Sun Liangpeng,Jiang Zhe,Gao Lixin,et al. Synthesis and Protein Tyrosine Phosphatase 1B Inhibitory Activity of Novel Chalcone Derivatives Containing 3,4-Dihydroquinolin-2(1H)-one Moiety[J]. CHINESE JOURNAL OF ORGANIC CHEMISTRY,2012,32(11):2108-2114. |
| APA | Sun Liangpeng.,Jiang Zhe.,Gao Lixin.,Li Yingzhe.,Sun Liyun.,...&Piao, Huri.(2012).Synthesis and Protein Tyrosine Phosphatase 1B Inhibitory Activity of Novel Chalcone Derivatives Containing 3,4-Dihydroquinolin-2(1H)-one Moiety.CHINESE JOURNAL OF ORGANIC CHEMISTRY,32(11),2108-2114. |
| MLA | Sun Liangpeng,et al."Synthesis and Protein Tyrosine Phosphatase 1B Inhibitory Activity of Novel Chalcone Derivatives Containing 3,4-Dihydroquinolin-2(1H)-one Moiety".CHINESE JOURNAL OF ORGANIC CHEMISTRY 32.11(2012):2108-2114. |
入库方式： OAI收割
来源：上海药物研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。