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学科主题: 生命有机化学
题名: Tuning the Acyclic Ether Moiety of Anticancer Agent AA005 with Conformationally Constrained Fragments
其他题名: 利用构象限制片段调节抗癌活性AA005的中间醚键区
作者: Liu HX(刘海侠) ; Shao F(邵飞) ; Li GQ(李纲琴) ; Xun GL(寻国良) ; Yao ZJ(姚祝军)
通讯作者: 姚祝军
刊名: Chem.-Eur. J.
发表日期: 2008
卷: 14, 期:28, 页:8632-8639
收录类别: SCI
部门归属: 上海有机化学研究所
英文摘要: A new series of anticancer annonaceous acetogenin mimetics were designed, synthesized, and evaluated based on our previously developed compound AA005, in which a variety of conformationally constrained fragments were introduced. Parallel syntheses of all new compounds were accomplished by replacement of the acyclic bis-ether functionality of AA005 with certain conformationally constrained fragments. Slight effects to the anticancer activity were exerted by altering stereochemistries in the middle modification region. Similar to AA005, most newly synthesized mimetics were found to exhibit potent activities against breast cancer cells, and showed satisfactory selectivities between cancerous and non-cancerous cells. An NN'-di-methyl bis-amide compound 67 exhibits 30 times more potency against MDA-MB-468 cells than its parent molecule AA005. This study indicates that the introduction of appropriate conformational constraints is a useful optimizing tool for this class of anticancer agents. Successes in the bis-amide analogues of AA005 make this unique class of anticancer agents much simpler and more flexible for future further developments.
语种: 英语
相关网址: 查看原文
WOS记录号: WOS:000260035900025
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内容类型: 期刊论文
URI标识: http://ir.sioc.ac.cn/handle/331003/21107
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:
Liu HX,Shao F,Li GQ,et al. Tuning the Acyclic Ether Moiety of Anticancer Agent AA005 with Conformationally Constrained Fragments[J]. Chem.-Eur. J.,2008,14(28):8632-8639.
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