New molecular entities and structure–activity relationships of drugs designed by the natural product derivatization method from 2010 to 2018

An important concept, the natural product derivatization method, was introduced and defined to comprehensively evaluate the significance of natural product derivatization in the design and development of pharmaceutical molecules. Therefore, based on the analysis of 464 new molecular entities registered for drugs worldwide from 2010 to 2018, the source, action mode, proportion of new active ingredients contained in “NP (natural product)” and “ND (natural product derivatives),” and structure–activity relationships were reviewed. Finally, the prospect of this method in the field of drug design is discussed.