Bromophenols as inhibitors of protein tyrosine phosphatase 1B with antidiabetic properties
文献类型：期刊论文
| 作者 | Shi, Dayong1; Li, Jing1 ; Jiang, Bo1; Guo, Shuju1; Su, Hua1; Wang, Tao2
|
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2012-04-15 |
| 卷号 | 22期号:8页码:2827-2832 |
| 关键词 | Bromophenol derivatives Protein tyrosine phosphatase 1B Diarylmethane Antidiabetic activities |
| ISSN号 | 0960-894X |
| 通讯作者 | Shi, DY (reprint author), Chinese Acad Sci, Inst Oceanol, Qingdao 266071, Peoples R China. |
| 英文摘要 | A series of bromophenol derivatives were synthesized and evaluated as protein tyrosine phosphatase 1B (PTP1B) inhibitors in vitro and in vivo based on bromophenol 4e (IC50 = 2.42 mu mol/ L), which was isolated from red algae Rhodomela confervoides. The results showed that all of the synthesized compounds displayed weak to good PTP1B inhibition at tested concentration. Among them, highly brominated compound 4g exhibited promising inhibitory activity against PTP1B with IC50 0.68 mu mol/L, which was approximately fourfold more potent than lead compound 4e. Further, compound 4g demonstrated high selectivity against other PTPs (TCPTP, LAR, SHP-1 and SHP-2). More importantly, in vivo antidiabetic activities investigations of compound 4g also demonstrated inspiring results. (C) 2012 Elsevier Ltd. All rights reserved. |
| 学科主题 | Chemistry, Medicinal ; Chemistry, Organic |
| 收录类别 | SCI |
| 原文出处 | 10.1016/j.bmcl.2012.02.074 |
| 语种 | 英语 |
| WOS记录号 | WOS:000302768200039 |
| 公开日期 | 2013-09-24 |
| 源URL | [http://ir.qdio.ac.cn/handle/337002/12215]  |
| 专题 | 海洋研究所_海洋生物技术研发中心 海洋研究所_实验海洋生物学重点实验室 |
| 作者单位 | 1.Chinese Acad Sci, Inst Oceanol, Qingdao 266071, Peoples R China 2.China Pharmaceut Univ, Jiangsu Ctr Drug Screening, Nanjing 210009, Peoples R China |
| 推荐引用方式 GB/T 7714 | Shi, Dayong,Li, Jing,Jiang, Bo,et al. Bromophenols as inhibitors of protein tyrosine phosphatase 1B with antidiabetic properties[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2012,22(8):2827-2832. |
| APA | Shi, Dayong,Li, Jing,Jiang, Bo,Guo, Shuju,Su, Hua,&Wang, Tao.(2012).Bromophenols as inhibitors of protein tyrosine phosphatase 1B with antidiabetic properties.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,22(8),2827-2832. |
| MLA | Shi, Dayong,et al."Bromophenols as inhibitors of protein tyrosine phosphatase 1B with antidiabetic properties".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 22.8(2012):2827-2832. |
入库方式： OAI收割
来源：海洋研究所
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