Repurposing of artemisinin-type drugs for the treatment of acute leukemia

Cancer treatment represents an unmet challenge due to the development of drug resistance and severe side effects of chemotherapy. Artemisinin (ARS)-type compounds exhibit excellent antimalarial effects with few side effects and drug-resistance. ARS and its derivatives were also reported to act against various tumor types in vitro and in vivo, including acute leukemia. Therefore, ARS-type compounds may be exquisitely suitable for repurposing in leukemia treatment. To provide comprehensive clues of ARS and its derivatives for acute leukemia treatment, their molecular mechanisms are discussed in this review. Five monomeric molecules and 72 dimers, trimers and hybrids based on the ARS scaffold have been described against acute leukemia. The modes of action involve anti-angiogenic, anti-metastatic and growth inhibitory effects. These properties make ARS-type compounds as potential candidates for the treatment of acute leukemia. Still, more potent and target-selective ARStype compounds need to be developed.

Automated summary

Cancer treatment is a challenge due to drug resistance and chemotherapy side effects. Artemisinin-type compounds have shown potential for acute leukemia treatment with anti-angiogenic, anti-metastatic, and growth inhibitory effects. More potent and target-selective compounds based on ARS scaffold are needed for further development.