Due to the clinical success and limitations of platinum-based anticancer drugs, there has been considerable interest in the development of new therapeutic agents based upon other transition metals, in particular ruthenium. There have now been many studies demonstrating the anticancer and antimicrobial properties of kinetically-inert polypyridylruthenium(II) complexes. This review showcases the diverse range of polypyridylruthenium complexes that exhibit significant biological activity, and discusses the relationship between their chemical structure and biological processing (cellular uptake and localisation) in eukaryotic cells. Perhaps more importantly, this review also highlights several recent studies that have shown kinetically-inert polypyridylruthenium(II) complexes can exhibit anticancer activity in in vivo trials – studies that provide the “proof of concept” that this class of metal-based agent has real clinical potential.

由于铂类抗癌药的临床成功和局限性，人们对基于其他过渡金属（尤其是钌）的新型治疗剂的开发抱有浓厚兴趣。现在已经有许多研究证明了动力学惰性的聚吡啶钌（II）配合物的抗癌和抗菌性能。这篇综述展示了具有显着生物学活性的聚吡啶钌复合物的各种范围，并讨论了其化学结构与真核细胞中生物加工（细胞摄取和定位）之间的关系。也许更重要的是，本综述还着重介绍了几项最近的研究，这些研究表明，动力学惰性的聚吡啶钌（II）复合物在体外具有抗癌活性。体内试验–提供“概念验证”的研究，表明此类金属基药物具有真正的临床潜力。