Regio-controlled synthesis of unsymmetrical pyrazine-fused sinomenine derivatives and discriminate substitution effects on TNF-alpha inhibitory activity
文献类型：期刊论文
| 作者 | Zhou, TT; Hou, J; Wang, M; Ma, LY; Wu, LL; Wang, SZ; Sun, B; Yao, ZJ |
| 刊名 | TETRAHEDRON
 |
| 出版日期 | 2014 |
| 卷号 | 70期号:35页码:5475-5482 |
| 关键词 | Sinomenine Pyrazine Regio-controlled synthesis Structure-activity relationship Tumor necrosis factor-alpha (TNF-alpha) |
| 通讯作者 | Sun, B (reprint author), Chinese Acad Sci, Shanghai Inst Biol Sci, Shanghai Inst Biochem & Cell Biol, Shanghai 200031, Peoples R China.,bsun@sibs.ac.cn ; yaoz@nju.edu.cn |
| 英文摘要 | A unified regio-controlled synthetic protocol combined with the use of Suzuki couplings, in a diverse fashion, has been developed and successfully applied to the synthesis of various pairs of unsymmetrical pyrazine-fused derivatives of sinomenine, a natural immunemodulating alkaloid. Introduction of two vicinal aromatic substituents to the pyrazine functionality resulted in significant improvement of TNF-alpha inhibitory activity, and a number of new derivatives exhibited even higher inhibition rate than that of positive control SB202190. In addition, discriminate but complicated substitution effects of these sinomenine-pyrazine hybrids have been observed on tumor necrosis factor-alpha (TNF-alpha) inhibitory activity. (C) 2014 Elsevier Ltd. All rights reserved. |
| 学科主题 | Chemistry |
| 类目[WOS] | Chemistry, Organic |
| 关键词[WOS] | DRUG DISCOVERY ; EXPRESSION ; CELLS |
| 收录类别 | SCI |
| 语种 | 英语 |
| WOS记录号 | WOS:000340336000014 |
| 版本 | 出版稿 |
| 源URL | [http://202.127.25.143/handle/331003/270]  |
| 专题 | 上海生化细胞研究所_上海生科院生化细胞研究所 |
| 推荐引用方式 GB/T 7714 | Zhou, TT,Hou, J,Wang, M,et al. Regio-controlled synthesis of unsymmetrical pyrazine-fused sinomenine derivatives and discriminate substitution effects on TNF-alpha inhibitory activity[J]. TETRAHEDRON,2014,70(35):5475-5482. |
| APA | Zhou, TT.,Hou, J.,Wang, M.,Ma, LY.,Wu, LL.,...&Yao, ZJ.(2014).Regio-controlled synthesis of unsymmetrical pyrazine-fused sinomenine derivatives and discriminate substitution effects on TNF-alpha inhibitory activity.TETRAHEDRON,70(35),5475-5482. |
| MLA | Zhou, TT,et al."Regio-controlled synthesis of unsymmetrical pyrazine-fused sinomenine derivatives and discriminate substitution effects on TNF-alpha inhibitory activity".TETRAHEDRON 70.35(2014):5475-5482. |
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