Discovery of 1,3-diphenyl-1H-pyrazole derivatives containing rhodanine-3-alkanoic acid groups as potential PTP1B inhibitors
文献类型：期刊论文
| 作者 | Sun, Liangpeng3; Wang, Peipei1 ; Xu, Lili2; Gao, Lixin1; Li, Jia1; Piao, Huri2
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2019-05-15 |
| 卷号 | 29期号:10页码:1187-1193 |
| 关键词 | PTP1B inhibitor 1,3-Diphenyl-1H-pyrazole Rhodanine-3-alkanoic acid |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2019.03.023 |
| 通讯作者 | Li, Jia(jli@simm.ac.cn) ; Piao, Huri(piaohr@ybu.edu.cn) |
| 英文摘要 | Two series of 1,3-diphenyl-1H-pyrazole derivatives containing rhodanine-3-alkanoic acid groups were identified as competitive protein tyrosine phosphatase 1B (PTP1B) inhibitors. Among the compounds studied, IIIv was found to have the best in vitro inhibition activity against PTP1B (IC50 = 0.67 +/- 0.09 mu M) and the best selectivity (9-fold) between PTP1B and T-cell protein tyrosine phosphatase (TCPTP). Molecular docking studies demonstrated that compounds IIIm, IIIv and IVg could occupy simultaneously at both the catalytic site and the adjacent pTyr binding site. These results provide novel lead compounds for the design of inhibitors of PTP1B as well as other PTPs. |
| WOS关键词 | TYROSINE-PHOSPHATASE 1B ; INSULIN-RECEPTOR ; OBESITY ; IDENTIFICATION ; SENSITIVITY ; RESISTANCE ; RHODANINE ; BEARING |
| 资助项目 | National Natural Science Foundation of China[81460524] ; National Natural Science Foundation of China[81773779] ; Education Department of Jilin Province Scientific Research Fund Project, China[2015-50] ; Edanz Group China |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000463383800007 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/290104]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Li, Jia; Piao, Huri |
| 作者单位 | 1.Chinese Acad Sci, Natl Ctr Drug Screening, Shanghai Inst Mat Med, Shanghai Inst Biol Sci, Shanghai 201203, Peoples R China 2.Yanbian Univ, Key Lab Nat Resources Changbai Mt & Funct Mol, Minist Educ, Coll Pharm, Yanji 133000, Peoples R China 3.Yanbian Univ, Coll Med, Yanji 133000, Peoples R China |
| 推荐引用方式 GB/T 7714 | Sun, Liangpeng,Wang, Peipei,Xu, Lili,et al. Discovery of 1,3-diphenyl-1H-pyrazole derivatives containing rhodanine-3-alkanoic acid groups as potential PTP1B inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2019,29(10):1187-1193. |
| APA | Sun, Liangpeng,Wang, Peipei,Xu, Lili,Gao, Lixin,Li, Jia,&Piao, Huri.(2019).Discovery of 1,3-diphenyl-1H-pyrazole derivatives containing rhodanine-3-alkanoic acid groups as potential PTP1B inhibitors.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,29(10),1187-1193. |
| MLA | Sun, Liangpeng,et al."Discovery of 1,3-diphenyl-1H-pyrazole derivatives containing rhodanine-3-alkanoic acid groups as potential PTP1B inhibitors".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 29.10(2019):1187-1193. |
入库方式： OAI收割
来源：上海药物研究所
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