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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
ISSN0365-6233
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
DOI10.1002/ardp.201100373
URL查看原文
收录类别SCI ; IC
语种英语
WOS记录号WOS:000305123700004
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被引频次:25[WOS]   [WOS记录]     [WOS相关记录]
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
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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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