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化学进展 2006, Vol. 18 Issue (06): 734-742 前一篇   后一篇

• 综述与评论 •

多样性导向的“类天然产物”化合物库合成*

刘钢1*;李裕林1;南发俊2**   

  1. 1.兰州大学功能有机分子国家重点实验室 有机化学研究所 兰州 730000;2. 中国科学院上海生命科学院 上海药物研究所国家新药筛选中心 上海 201203
  • 收稿日期:2005-12-01 修回日期:2006-03-01 出版日期:2006-06-24 发布日期:2006-06-24
  • 通讯作者: 南发俊
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Diversity-Oriented Synthesis of Natural Product-Like Libraries

Gang Liu1*; Yulin Li1; Fajun Nan2**   

  1. 1.Institute of Organic Chemistry,State Key Laboratory of Applied Organic Chemistry, Lanzhou University, Lanzhou 730000, China; 2. Chinese National Center for Drug Screening, Shanghai Insitute of Materia Medica, Shanghai Institutes of Biological Sciences, Shanghai 201203, China
  • Received:2005-12-01 Revised:2006-03-01 Online:2006-06-24 Published:2006-06-24
  • Contact: Fajun Nan
天然产物是药物发现中先导化合物的重要来源。高通量筛选技术的发展和近年来化学生物学研究的深入, 对拓展天然产物与活性相关的”化学空间”提出了新要求。用多样性导向合成方法建立骨架多样、构造复杂、立体化学多样性的“类天然产物”化合物库进行生物学相关研究, 并以此为基础发现药物先导化合物正在成为一种趋势。在此过程中，发展具有立体选择性和区域选择性，能够广泛应用于多种底物的有机化学反应起着关键作用。
关键词： 多样性导向合成, “类天然产物”化合物库, 目标导向合成
Natural products provide the most important sources of lead compounds in drug discovery. With the development of high-throughput screening (HTS) technology and in depth studies in chemical biology, exploring pharmaceutically relevant chemical space of natural products is vital. Employing diversity-oriented synthesis (DOS) to construct skeletally complex natural product-like libraries and using it in the studies of chemical biology and lead discovery is becoming a tendency. The development of exceptionally efficient, stereoselective, and chemoselective reactions that can be applied to a wide range of substrates play key roles.
Key words: diversity-oriented synthesis (DOS), natural product-like libraries, target-oriented synthesis

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