| Total synthesis of bis-（2,3-dibromo-4,5-dihydroxyphenyl）-methane as potent PTP1B inhibitor |
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| 作者姓名： | Jing Li ;Shu Ju Guo ;Hua Su ;Li Jun Han ;Da Yong Shi |
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| 作者单位： | a Institute of Oceanology, Chinese Academy of Sciences, Qingdao 266071, China;b Graduate School of the Chinese Academy of Sciences, Beijing 100039, China |
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| 基金项目： | Acknowledgments We thank to the National Center for Drug Screening （Shanghai, PR China） for supplying data on PTPI B inhibitory activities of compounds. This work was supported by the National 863 projects （Nos. 2007AA09Z410 and 2007AA091604）. |
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| 摘 要： | Protein tyrosine phosphatase 1B （PTP1B） plays an important role as a negative regulator and has been proved to be an effective target for the treatment of type 2 diabetes mellitus. Bis-（2,3-dibromo-4,5-dihydroxyphenyl）-methane 7 was first reported as a natural bromophenol with significant inhibition against PTP1B which was isolated from red algae Rhodomela conrervoides. Intrigued by its astonishing activity （IC50 = 2.4 μmol/L）, compound 7 was synthesized with the overall yield of 24% and evaluated for its PTPIB inhibitory activity compared with natural compound.
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| 关 键 词： | 蛋白络氨酸磷酸酶1B 合成方法 化学 抑制剂 |
Total synthesis of bis-(2,3-dibromo-4,5-dihydroxyphenyl)-methane as potent PTP1B inhibitor |
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| Jing Li,;Shu Ju Guo,;Hua Su,;Li Jun Han,;Da Yong Shi.Total synthesis of bis-(2,3-dibromo-4,5-dihydroxyphenyl)-methane as potent PTP1B inhibitor[J].Chinese Chemical Letters,2008,19(11):1290-1292. |
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| Authors: | Jing Li Shu Ju Guo Hua Su Li Jun Han Da Yong Shi |
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| Institution: | a Institute of Oceanology, Chinese Academy of Sciences, Qingdao 266071, China;b Graduate School of the Chinese Academy of Sciences, Beijing 100039, China |
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| Abstract: | Protein tyrosine phosphatase 1B (PTPI B) plays an important role as a negative regulator and has been proved to be an effective target for the treatment of type 2 diabetes mellitus.Bis-(2,3-dibromo-4,5-dihydroxyphenyl)-methane 7 was first reported as a natural bromopbenol with significant inhibition against PTP1B which was isolated from red algae Rhodomela confervoides.Intrigued by its astonishing activity (IC50=2.4 μmol/L),compound 7 was synthesized with the overall yield of 24% and evaluated for its PTP1B inhibitory activity compared with natural compound. |
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| Keywords: | Bromophenol Bis-(2 3-dibromo-405-dihydroxyphenyl)-methane PTP1B inhibitor Total synthesis |
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