RESUMEN
Artemisinin is the crucial ingredient of artemisia annua, a traditional Chinese medicine used for the therapy of malaria in China for hundreds of years. In recent years, the anticancer properties of artemisinin and its derivatives have also been reported. This review has summarized the research and development of artemisinin and its derivatives as anticancer agents, which included both natural and synthetic monomers as well as their dimers. In addition, it highlights the antitumor effects of artemisinin and its derivatives after site-modification or after transformation to a nano-delivery system. Moreover, we have further explored their potential mechanisms of action and also discussed the clinical trials of ARTs used to treat cancer, which will facilitate in further development of novel anticancer drugs based on the scaffold of artemisinin.