Cancer is the leading cause of human death which seriously threatens human life. The
antimalarial drug artemisinin and its derivatives have been discovered with considerable anticancer properties. Simultaneously, a variety of target-selective
artemisinin-related compounds with high efficiency have been discovered. Many researches indicated that
artemisinin-related compounds have cytotoxic effects against a variety of
cancer cells through pleiotropic effects, including inhibiting the proliferation of
tumor cells, promoting apoptosis, inducing cell cycle arrest, disrupting
cancer invasion and
metastasis, preventing angiogenesis, mediating the
tumor-related signaling pathways, and regulating tumor microenvironment. More importantly,
artemisinins demonstrated minor side effects to normal cells and manifested the ability to overcome multidrug-resistance which is widely observed in
cancer patients. Therefore, we concentrated on the new advances and development of
artemisinin and its derivatives as potential
antitumor agents in recent 5 years. It is our hope that this review could be helpful for further exploration of novel
artemisinin-related
antitumor agents.