Anticancer agents play a pivotal role in cancer treatment. However, most of the anticancer drugs currently used in the clinics have a severe anticancer scenario, as well as low specificity and fatal side effects. Thus, there is an urgent demand to develop novel drugs with great efficacy, high specificity, and low side effects. Artemisinin and its semisynthetic derivatives are mainstays of chemotherapy against malaria, and artemisinin‐based compounds, especially artemisinin‐derived dimers, also exhibit excellent in vitro and in vivo anticancer activity. The structure–activity relationship (SAR) demonstrated that the linker between the two artemisinin moieties influenced the anticancer activity significantly; so, the rational design of the linker may provide valuable therapeutic intervention for the treatment of cancer. This review outlines the potential anticancer activity of artemisinin‐derived dimers tethered by different linkers. The SARs, as well as mechanisms of action, are discussed to provide insights for the rational design of more effective dimers.

中文翻译：

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青蒿素衍生的二聚体作为潜在的抗癌剂：当前的发展、作用机制和构效关系

抗癌药物在癌症治疗中发挥着关键作用。然而，目前临床上使用的大多数抗癌药物都具有严重的抗癌场景，以及特异性低和致命的副作用。因此，迫切需要开发具有高疗效、高特异性和低副作用的新型药物。青蒿素及其半合成衍生物是抗疟疾化疗的中流砥柱，青蒿素类化合物，尤其是青蒿素衍生的二聚体，也表现出优异的体外和体内抗癌活性。构效关系（SAR）表明，两个青蒿素部分之间的接头显着影响了抗癌活性；因此，接头的合理设计可能为癌症的治疗提供有价值的治疗干预。本综述概述了由不同接头连接的青蒿素衍生二聚体的潜在抗癌活性。讨论了 SAR 以及作用机制，以便为更有效的二聚体的合理设计提供见解。