| Design, Synthesis, and Biological Evaluation of Bromophenol Derivatives as Protein Tyrosine Phosphatase 1B Inhibitors | |
| Jiang, Bo; Shi, Dayong; Cui, Yongchao; Guo, Shuju; Shi, DY (reprint author), Chinese Acad Sci, R&D Ctr Marine Biotechnol, Inst Oceanol, Qingdao, Peoples R China. | |
| 2012-06-01 | |
| 发表期刊 | ARCHIV DER PHARMAZIE
 |
| ISSN | 0365-6233 |
| 卷号 | 345期号:6页码:444-453 |
| 文章类型 | Article |
| 摘要 | 3-Bromo-4,5-bis(2,3-dibromo-4,5-dihydroxybenzyl)-1,2-benzenediol (BDB) is a bromophenol purified from the marine red alga Rhodomela confervoides and exhibits potent protein tyrosine phosphatase 1B (PTP1B) inhibition (IC50?=?1.7?mu mol/L). In an effort to improve the PTP1B inhibitory activity, a series of derivatives were designed, synthesized, and evaluated in vitro. The preliminary structureactivity relationship indicated that the tricyclic scaffold and multi-bromine atoms (four to five) attached to the aryl rings are important for PTP1B inhibition. Among these, compound 26 exhibited remarkable inhibitory activity against PTP1B with an IC50 of 0.89 mu mol/L, which was approximately two-fold more potent than the initial lead compound BDB. |
| 关键词 | Bromophenol Protein Tyrosine Phosphatase 1b Inhibitor Structure-activity Relationship Type 2 Diabetes Mellitus |
| 学科领域 | Chemistry, Medicinal ; Chemistry, Multidisciplinary ; Pharmacology & Pharmacy |
| DOI | 10.1002/ardp.201100373 |
| URL | 查看原文 |
| 收录类别 | SCI ; IC |
| 语种 | 英语 |
| WOS记录号 | WOS:000305123700004 |
| 引用统计 | |
| 文献类型 | 期刊论文 |
| 条目标识符 | http://ir.qdio.ac.cn/handle/337002/12218 |
| 专题 | 海洋生物技术研发中心 |
| 通讯作者 | Shi, DY (reprint author), Chinese Acad Sci, R&D Ctr Marine Biotechnol, Inst Oceanol, Qingdao, Peoples R China. |
| 作者单位 | Chinese Acad Sci, R&D Ctr Marine Biotechnol, Inst Oceanol, Qingdao, Peoples R China |
| 推荐引用方式 GB/T 7714 | Jiang, Bo,Shi, Dayong,Cui, Yongchao,et al. Design, Synthesis, and Biological Evaluation of Bromophenol Derivatives as Protein Tyrosine Phosphatase 1B Inhibitors[J]. ARCHIV DER PHARMAZIE,2012,345(6):444-453. |
| APA | Jiang, Bo,Shi, Dayong,Cui, Yongchao,Guo, Shuju,&Shi, DY .(2012).Design, Synthesis, and Biological Evaluation of Bromophenol Derivatives as Protein Tyrosine Phosphatase 1B Inhibitors.ARCHIV DER PHARMAZIE,345(6),444-453. |
| MLA | Jiang, Bo,et al."Design, Synthesis, and Biological Evaluation of Bromophenol Derivatives as Protein Tyrosine Phosphatase 1B Inhibitors".ARCHIV DER PHARMAZIE 345.6(2012):444-453. |
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