Modification of poorly bioactive sinomenine into more potent immunosuppressive agents by embedding of drug-like fragments
文献类型：期刊论文
| 作者 | Lou, YT; Zhou, HB; Zou, J; Yan, LC; Bi, EG; Sun, B; Yao, ZJ |
| 刊名 | TETRAHEDRON LETTERS
 |
| 出版日期 | 2010 |
| 卷号 | 51期号:3页码:485-488 |
| 关键词 | Sinomenine Alkaloid Drug fragment Modification Immunomodulating activity |
| 通讯作者 | Sun, B (reprint author), Chinese Acad Sci, Shanghai Inst Biol Sci, Shanghai Inst Biochem & Cell Biol, 219 Yueyong Rd, Shanghai 200031, Peoples R China.,bingsun@sib.ac.cn ; yaoz@mail.sioc.ac.cn |
| 英文摘要 | Embedment of drug-like heterocyclic moieties was Successfully employed in the novel modification of the readily available but poorly bioactive natural alkaloid sinomenine. Application of the newly proposed approach afforded a number of more potent sinomenine-like molecules with a significantly high hit rate. Among these new analogous, up to 500-fold increase of in vitro immunosuppressive activity was achieved. Further biological experiments of representative compound 4b indicated that it might inhibit NF-kappa B activation induced by TNF-alpha in a dose dependent way and showed remarkable in vivo treatment effects against the mouse experimental autoimmune uveoretinitis (EAU) disease models. (C) 2009 Elsevier Ltd. All rights reserved. |
| 学科主题 | Chemistry |
| 类目[WOS] | Chemistry, Organic |
| 关键词[WOS] | EXPERIMENTAL AUTOIMMUNE UVEORETINITIS ; CELLS ; MICE ; EXPRESSION ; MODEL ; EAU |
| 收录类别 | SCI |
| 语种 | 英语 |
| WOS记录号 | WOS:000274477300006 |
| 版本 | 出版稿 |
| 源URL | [http://202.127.25.143/handle/331003/985]  |
| 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 | Lou, YT,Zhou, HB,Zou, J,et al. Modification of poorly bioactive sinomenine into more potent immunosuppressive agents by embedding of drug-like fragments[J]. TETRAHEDRON LETTERS,2010,51(3):485-488. |
| APA | Lou, YT.,Zhou, HB.,Zou, J.,Yan, LC.,Bi, EG.,...&Yao, ZJ.(2010).Modification of poorly bioactive sinomenine into more potent immunosuppressive agents by embedding of drug-like fragments.TETRAHEDRON LETTERS,51(3),485-488. |
| MLA | Lou, YT,et al."Modification of poorly bioactive sinomenine into more potent immunosuppressive agents by embedding of drug-like fragments".TETRAHEDRON LETTERS 51.3(2010):485-488. |
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