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有机化学
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有机化学 ›› 2012, Vol. 32 ›› Issue (01): 1-12.DOI: 10.6023/cjoc1110141 上一篇    下一篇

综述与进展

Englerin A 的全合成及其类似物生物活性的研究进展

卢云宇a,b, 姚和权a, 孙炳峰b   

  1. a 中国药科大学药学院 南京 210009;
    b 中国科学院上海有机化学研究所 中国科学院天然产物有机合成化学重点实验室 上海 200032
  • 收稿日期:2011-10-14 修回日期:2011-11-17 发布日期:2011-11-17
  • 通讯作者: 孙炳峰 E-mail:bfsun@sioc.ac.cn
  • 基金资助:

    国家自然科学基金(Nos. 20902101, 21172246)和国家重点基础研究发展规划(973 计划, No. 2010CB833206)资助项目.

Progresses in Total Synthesis of Englerin A and Biological Evaluations of Its Analogues

Lu Yunyua,b, Yao Hequana, Sun Bingfengb   

  1. a School of Pharmacy, China Pharmaceutical University, Nanjing 210009;
    b Key Laboratory of Synthetic Chemistry of Natural Substances, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai 200032
  • Received:2011-10-14 Revised:2011-11-17 Published:2011-11-17
  • Contact: Bingfeng Sun E-mail:bfsun@sioc.ac.cn
  • Supported by:

    Project supported by the National Natural Science Foundation of China (Nos. 20902101, 21172246) and the National Basic Research Program of China (973 Program, No. 2010CB833206).

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Englerin A 是一种从大戟属植物Phyllanthus engleri 中分离得到的含有氧桥结构的愈创木烷类倍半萜, 对肾癌细胞表现出很高的抑制活性和选择性. 综述了englerin A 的全合成及其初步构效关系的研究进展. 在合成部分, 对各个合成路线的特点, 尤其对氧杂三环骨架的构建过程进行了重点讨论.

关键词: englerin A, 全合成, 生物活性, 研究进展

Englerin A is an oxo-bridged guaiane-type sesquiterpenoid isolated from Phyllanthus engleri, and displays potent and highly selective inhibitory activities against renal cancer cell lines. In this review, the recent progresses since its disclosure in the total synthesis of englerin A and biological evaluations of its analogues are summarized, with an emphasis on the strategies of the synthetic routes, particularly in regards to the construction of oxatricyclic ring system.

Key words: englerin A, total synthesis, biological evaluation, progress