Dipartimento di Scienze e Innovazione Tecnologica, Università del Piemonte Orientale, Viale Michel 11, Alessandria, Italy.
UCD School of Chemistry, University College Dublin, Belfield, Dublin 4, Ireland.
Dalton Trans. 2022 Feb 8;51(6):2121-2134. doi: 10.1039/d1dt03886a.
Platinum(II)-based drugs are widely used for the treatment of solid tumors, especially in combination protocols. Severe side effects and occurrence of resistance are the major limitations to their clinical use. To overcome these drawbacks, a plethora of Pt(IV) derivatives, acting as anticancer prodrugs, have been designed, synthesized and preclinically (often only ) tested. Here, we summarize the recent progress in the development and understanding of the chemical properties and biochemical features of these Pt(IV) prodrugs, especially those containing bioactive molecules as axial ligands, acting as multi-functional agents. Even though no such prodrugs have been yet approved for clinical use, many show encouraging pharmacological profiles. Thus, a better understanding of their features is a promising approach towards improving the available Pt-based anticancer agents.
基于铂(II)的药物被广泛用于治疗实体瘤，特别是在联合方案中。严重的副作用和耐药性的发生是其临床应用的主要限制。为了克服这些缺点，设计、合成并进行了大量的 Pt(IV)衍生物作为抗癌前药的临床前（通常仅）测试。在这里，我们总结了这些 Pt(IV)前药的化学性质和生化特性的最新进展和理解，特别是那些含有作为轴向配体的生物活性分子的前药，作为多功能试剂。尽管这些前药尚未被批准用于临床使用，但许多前药显示出令人鼓舞的药理学特征。因此，更好地了解它们的特征是改进现有基于铂的抗癌药物的一种很有前途的方法。
