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学科主题: 生命有机化学
题名: Modification of poorly bioactive sinomenine into more potent immunosuppressive agents by embedding of drug-like fragments
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
作者: LOU YANGTONG ; ZHOU HAIBIN ; ZOU JIA ; YAN LINGCHEN ; BI ENGUAN ; Sun B(孙兵) ; Yao ZJ(姚祝军)
通讯作者: 孙兵 ; 姚祝军
刊名: Tetrahedron Lett.
发表日期: 2010-01-01
卷: 51, 期:3, 页:485-488
收录类别: SCI
部门归属: 中国科学院上海有机化学研究所; 中国科学院上海生命科学研究院
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.
语种: 英语
相关网址: 查看原文
WOS记录号: WOS:000274477300006
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内容类型: 期刊论文
URI标识: http://ir.sioc.ac.cn/handle/331003/21145
Appears in Collections:生命有机化学国家重点实验室_期刊论文

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Recommended Citation:
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.
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