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化学进展 2009, Vol. 21 Issue (01): 47-54 前一篇   后一篇

• 中药研究专刊 •

活性天然产物和结构多样性类天然产物的合成

杨震*   

  1. (北京大学化学学院 北京 100871)
  • 收稿日期:2008-10-10 修回日期:1900-01-01 出版日期:2009-01-24 发布日期:2009-01-25
  • 通讯作者: 杨震 E-mail:zyang@pku.edu.cn

Syntheses of Biological Active Natural Products and Natural Product-Like Molecules

Yang Zhen*   

  1. (College of Chemistry, Peking University, Beijing 100871, China)
  • Received:2008-10-10 Revised:1900-01-01 Online:2009-01-24 Published:2009-01-25
  • Contact: Yang Zhen E-mail:zyang@pku.edu.cn

天然产物骨架的复杂性和丰富的官能团化赋予了天然产物类化合物独有的生物学活性,因此天然产物作为药物研究的先导化合物有其无法替代的独特性质,比如紫杉醇、红霉素和利福霉素帮助科学家们理解重要的生物过程。以往化学家对天然产物独有情钟,但仅仅以合成天然产物本身为最终目的。今天,化学家们开始利用传统的合成方法来制备结构多样性的类天然产物化合物。这种利用合成手段制备的小分子化合物在生物学的基础研究和药物研究中将起到关键的作用。

Natural products are the richest known source of small molecules that bind proteins with high specificity, thanks to millions of years of evolution and selection. Many natural products, such as Taxol, erythromycin and rifamycin have helped scientists to understand biological processes. Synthetic chemists have long been fascinated by natural products, but have until now focused on precisely copying what is available in nature. Recently, chemists have become aware that it is now possible to make "natural-product-like" compounds that are comparable to true natural products in size and complexity. When this insight is combined with the strategy of diversity oriented synthesis, which allows large numbers of compounds to be made quickly, it becomes possible to think of "evolving" our traditionally specific synthetic tools to synthesize "natural-product-like" molecules for probing the important biological events. The ability to find specific small molecule ligands that modulate the biological molecular functions would be extremely valuable both in basic research and in drug design.

Contents
1 Introduction
2 Diversity-oriented synthesis of guanacastepenes
3 Diversity-oriented oriented synthesis of neuraminidase inhibitors
4 Conclusion

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[1] 刘钢,李裕林,南发俊. 多样性导向的“类天然产物”化合物库合成*[J]. 化学进展, 2006, 18(06): 734-742.