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 ARS-type compounds need to be developed.

由于耐药性的发展和化学疗法的严重副作用，癌症治疗是一个尚未解决的挑战。青蒿素（ARS）类化合物具有优良的抗疟作用，副作用少，耐药性好。ARS 及其衍生物也被报道在体外和体内对各种肿瘤类型起作用，包括急性白血病。因此，ARS 型化合物可能非常适合重新用于白血病治疗。为了提供 ARS 及其衍生物用于急性白血病治疗的全面线索，本文讨论了它们的分子机制。已经描述了基于 ARS 支架的五种单体分子和 72 种二聚体、三聚体和杂合体来对抗急性白血病。作用方式包括抗血管生成、抗转移和生长抑制作用。这些特性使 ARS 型化合物成为治疗急性白血病的潜在候选者。尽管如此，仍需要开发更有效和目标选择性更强的 ARS 型化合物。