Synthesis of three bromophenols from red algae as PTP1B inhibitors
文献类型：CNKI期刊论文
| 作者 | Guo SJ(郭书举); Li J(李敬); Li T(李婷); Shi DY(史大永); Han LJ(韩丽君) |
| 发表日期 | 2011-01-15 |
| 出处 | Chinese Journal of Oceanology and Limnology
 |
| 关键词 | bromophenols synthesis PTP1B inhibitory activity |
| 英文摘要 | Bromophenols are a set of natural products widely distributed in seaweed, most of which exhibit interesting and useful biological activities. To develop a reliable and efficient synthetic route to these natural bromophenols, three of them, 3,4-dibromo-5-(2′-bromo-3′,4′- dihydroxy-6′-methoxymethyl- benzyl)-benzene-1,2-diol (compound 9), 3,4-dibromo-5-(2′-bromo-6′-ethoxy methyl-3′,4′-dihydroxybenzyl)- benzene-1,2-diol (compound 10), and 3-bromo-4-(3′-bromo-4′,5′-dihydroxy benzyl)-5-(ethoxymethyl)- benzene-1,2-diol (compound 14), isolated from red marine algae, have been synthesized in eight steps with an overall yield of 14.4%, 14.4%, and 18.2% respectively, via a practical approach employing bromination, Wolff-Kishner-Huang reduction and a Friedel-Crafts reaction as key steps. The protein tyrosine phosphatase 1B (PTP1B) inhibitory activities of the synthetic compounds were evaluated by the colorimetric assay. The results show that these compounds are moderate PTP1B inhibitors. The synthesis of these bromophenol derivatives makes in vivo studies of their structure-activity relationships and inhibition activity against PTP1B possible. |
| 文献子类 | CNKI期刊论文 |
| 资助机构 | Supported by the National Major Research Program of China (No.2009ZX09103-148) ; the National High Technology Research and Development Program of China (863 program) (Nos.2007AA09Z410,2007AA091604) |
| 卷 | v.29期:01页:70-76 |
| 语种 | 英文; |
| 分类号 | TQ464 |
| ISSN号 | 0254-4059 |
| 源URL | [http://ir.qdio.ac.cn/handle/337002/191842]  |
| 专题 | 中国科学院海洋研究所 |
| 作者单位 | 1.InstituteofOceanology,ChineseAcademyofSciences 2.GraduateUniversityoftheChineseAcademyofSciences |
| 推荐引用方式 GB/T 7714 | Guo SJ,Li J,Li T,et al. Synthesis of three bromophenols from red algae as PTP1B inhibitors. 2011. |
入库方式： OAI收割
来源：海洋研究所
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