Application of natural products derivatization method in the design of targeted anticancer agents from 2000 to 2018.

A concept, natural products derivatization method (NPDM), was introduced to assess the influence of natural products on the discovery of targeted anticancer agents. Subsequently, 106 new molecular entities (NMEs) for targeted anticancer agents from 2000 to 2018 were categorized and sorted into four types: ND (Natural Product Derivative), SND (Synthetic Natural Derived), B (Biological Macromolecule), S (Totally synthetic in origin). Furthermore, by setting molecular targeted agents (MTA), cellular targeted agents (CTA), vascular targeted agents (VTA) and immuno targeted agents (ITA) as study subject, ND category and SND category were reviewed from aspects including natural products source, action mechanism and their share in all NMEs in order to comprehensively evaluate the significance of NPDM in the design and development of targeted anticancer agents, and the prospects of this method was also put forward.