Iron chelators have long been a target of interest as anticancer agents. Iron is an important cellular resource involved in cell replication, metabolism and growth. Iron metabolism is modulated in cancer cells reflecting their increased replicative demands. Originally, iron chelators were first developed for use in iron overload disorders, however, their potential as anticancer agents has been gaining increasing interest. This is due, in part, to the downstream effects of iron depletion such as the inhibition of proliferation through ribonucleotide reductase activity. Additionally, some chelators form redox active metal complexes with iron resulting in the production of reactive oxygen species and oxidative stress. Newer synthetic iron chelators such as Deferasirox, Triapine and di-2-pyridylketone-4,4,-dimethyl-3-thiosemicrbazone (Dp44mt) have improved pharmacokinetic properties over the older chelator Deferoxamine. This review examines and discusses the various iron chelators that have been trialled for cancer therapy including both preclinical and clinical studies. The successes and shortcomings of each of the chelators and their use in combination therapies are highlighted and future potential in the cancer therapy world is considered.

铁螯合剂长期以来一直是作为抗癌剂的关注目标。铁是参与细胞复制、代谢和生长的重要细胞资源。铁代谢在癌细胞中受到调节，反映了它们增加的复制需求。最初，铁螯合剂首先被开发用于铁过载疾病，然而，它们作为抗癌剂的潜力越来越受到关注。这部分是由于铁消耗的下游效应，例如通过核糖核苷酸还原酶活性抑制增殖。此外，一些螯合剂与铁形成氧化还原活性金属络合物，导致产生活性氧和氧化应激。较新的合成铁螯合剂，例如 Deferasirox、Triapine 和 di-2-pyridylketone-4,4，-二甲基-3-氨基硫脲 (Dp44mt) 比旧的螯合剂去铁胺具有更好的药代动力学特性。本综述检查并讨论了各种已被试验用于癌症治疗的铁螯合剂，包括临床前和临床研究。强调了每种螯合剂的成功和缺点及其在联合治疗中的应用，并考虑了癌症治疗领域的未来潜力。