| Bromophenols as inhibitors of protein tyrosine phosphatase 1B with antidiabetic properties | |
Shi, Dayong1; Li, Jing1 ; Jiang, Bo1; Guo, Shuju1; Su, Hua1; Wang, Tao2; Shi, DY (reprint author), Chinese Acad Sci, Inst Oceanol, Qingdao 266071, Peoples R China.
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| 2012-04-15 | |
| 发表期刊 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
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| ISSN | 0960-894X |
| 卷号 | 22期号:8页码:2827-2832 |
| 文章类型 | Article |
| 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. |
| 关键词 | Bromophenol Derivatives Protein Tyrosine Phosphatase 1b Diarylmethane Antidiabetic Activities |
| 学科领域 | Chemistry, Medicinal ; Chemistry, Organic |
| DOI | 10.1016/j.bmcl.2012.02.074 |
| URL | 查看原文 |
| 收录类别 | SCI |
| 语种 | 英语 |
| WOS记录号 | WOS:000302768200039 |
| 引用统计 | |
| 文献类型 | 期刊论文 |
| 条目标识符 | http://ir.qdio.ac.cn/handle/337002/12215 |
| 专题 | 海洋生物技术研发中心 实验海洋生物学重点实验室 |
| 通讯作者 | Shi, DY (reprint author), Chinese Acad Sci, Inst Oceanol, Qingdao 266071, Peoples R China. |
| 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 |
| 第一作者单位 | 中国科学院海洋研究所 |
| 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.,...&Shi, DY .(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. |
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