Hong Benke, Luo Tuoping, Lei Xiaoguang
Beijing National Laboratory for Molecular Sciences, Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, Peking University, Beijing 100871, China.
Department of Chemical Biology, Peking University, Beijing 100871, China.
ACS Cent Sci. 2020 May 27;6(5):622-635. doi: 10.1021/acscentsci.9b00916. Epub 2020 Apr 22.
Late-stage diversification of natural products is an efficient way to generate natural product derivatives for drug discovery and chemical biology. Benefiting from the development of site-selective synthetic methodologies, late-stage diversification of natural products has achieved notable success. This outlook will outline selected examples of novel methodologies for site-selective transformations of reactive functional groups and inert C-H bonds that enable late-stage diversification of complex natural products. Accordingly, late-stage diversification provides an opportunity to rapidly access various derivatives for modifying lead compounds, identifying cellular targets, probing protein-protein interactions, and elucidating natural product biosynthetic relationships.
天然产物的后期多样化是生成用于药物发现和化学生物学的天然产物衍生物的有效方法。受益于位点选择性合成方法的发展,天然产物的后期多样化已取得显著成功。本展望将概述用于活性官能团和惰性C-H键的位点选择性转化的新型方法的选定实例,这些方法能够实现复杂天然产物的后期多样化。因此,后期多样化为快速获得各种衍生物提供了机会,可用于修饰先导化合物、识别细胞靶点、探究蛋白质-蛋白质相互作用以及阐明天然产物的生物合成关系。