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 YANGTONG ; ZHOU HAIBIN ; ZOU JIA ; YAN LINGCHEN ; BI ENGUAN ; Sun B(孙兵) ; Yao ZJ(姚祝军) |
| 刊名 | Tetrahedron Lett.
 |
| 出版日期 | 2010 |
| 卷号 | 51期号:3页码:485-488 |
| ISSN号 | 0040-4039 |
| 其他题名 | 通过接入药物碎片修饰低活性青藤碱来获得高活性的免疫抑制化合物 |
| 通讯作者 | 孙兵 ; 姚祝军 |
| 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 | 生命有机化学 |
| 收录类别 | SCI |
| 原文出处 | http://dx.doi.org/10.1016/j.tetlet.2009.11.019 |
| 语种 | 英语 |
| WOS记录号 | WOS:000274477300006 |
| 公开日期 | 2013-02-26 |
| 源URL | [http://202.127.28.38/handle/331003/21145]  |
| 专题 | 上海有机化学研究所_生命有机化学国家重点实验室 |
| 推荐引用方式 GB/T 7714 | LOU YANGTONG,ZHOU HAIBIN,ZOU JIA,et al. Modification of poorly bioactive sinomenine into more potent immunosuppressive agents by embedding of drug-like fragments[J]. Tetrahedron Lett.,2010,51(3):485-488. |
| APA | LOU YANGTONG.,ZHOU HAIBIN.,ZOU JIA.,YAN LINGCHEN.,BI ENGUAN.,...&姚祝军.(2010).Modification of poorly bioactive sinomenine into more potent immunosuppressive agents by embedding of drug-like fragments.Tetrahedron Lett.,51(3),485-488. |
| MLA | LOU YANGTONG,et al."Modification of poorly bioactive sinomenine into more potent immunosuppressive agents by embedding of drug-like fragments".Tetrahedron Lett. 51.3(2010):485-488. |
入库方式： OAI收割
来源：上海有机化学研究所
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