Guo Zongru
Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
Acta Pharm Sin B. 2017 Mar;7(2):119-136. doi: 10.1016/j.apsb.2016.06.003. Epub 2016 Nov 25.
Drug innovation is characterized by painstaking molecular-level syntheses and modifications as the basic components of research and development. Similarly, natural products are chemically tailored and modified based upon their structural and biological properties. To some extent, the modification of natural products is quite different from structure-based drug discovery. This review describes the general strategies and principles for the modification of natural products to drugs, as illustrated by several successful medicines that originated from natural products.
药物创新的特点是在分子水平上进行艰苦的合成和修饰,这是研发的基本组成部分。同样,天然产物也会根据其结构和生物学特性进行化学定制和修饰。在某种程度上,天然产物的修饰与基于结构的药物发现有很大不同。本综述描述了将天然产物修饰为药物的一般策略和原则,并以几种源自天然产物的成功药物为例进行说明。