Bakalova Adriana, Ruseva Nina, Cherneva Emiliya
Department of Chemistry, Faculty of Pharmacy, Medical University of Sofia, 2 Dunav Str., 1000 Sofia, Bulgaria.
Department of General and Inorganic Chemistry, University of Chemical Technology and Metallurgy, 8 Kliment Ohridsky Blvd., 1797 Sofia, Bulgaria.
Int J Mol Sci. 2025 Jun 28;26(13):6270. doi: 10.3390/ijms26136270.
The utilization of platinum complexes in medicine continues to be a prevalent treatment modality for diverse tumour types. However, it should be noted that certain platinum complexes are characterized by a high degree of toxicity. In recent years, there has been a focus among scientists on synthesizing "non-classic" platinum complexes, such as those with a -configuration, Pt(IV) complexes, and mixed ammine/amine platinum complexes, with the aim of reducing the toxic side effects of certain platinum complexes, including cisplatin. For instance, newly synthesized platinum complexes with a -configuration exhibited substantial cytotoxic activity which was comparable to that of the corresponding -isomers and cisplatin. This finding challenged the prevailing -geometry paradigm and prompted a re-evaluation of the structural activity relationships (SARs) of antitumour platinum complexes. It is widely accepted that Pt(IV) complexes act as prodrugs and release the active Pt(II) species. This property renders them promising candidates as anticancer drugs. Furthermore, it has been established that mixed ammine/amine platinum complexes are less toxic than cisplatin. In addition, compared to cisplatin, they have been observed to have equivalent or greater cytotoxic activity.
铂配合物在医学上的应用仍然是多种肿瘤类型普遍采用的治疗方式。然而,应当注意的是,某些铂配合物具有高度的毒性。近年来,科学家们专注于合成“非经典”铂配合物,如具有α-构型的配合物、Pt(IV)配合物以及混合氨/胺铂配合物,目的是降低某些铂配合物(包括顺铂)的毒副作用。例如,新合成的具有α-构型的铂配合物表现出相当大的细胞毒性活性,与相应的β-异构体和顺铂相当。这一发现挑战了普遍存在的β-几何构型范式,并促使人们重新评估抗肿瘤铂配合物的构效关系(SARs)。人们普遍认为Pt(IV)配合物作为前药发挥作用并释放出活性Pt(II)物种。这一特性使其成为有前景的抗癌药物候选物。此外,已经证实混合氨/胺铂配合物的毒性比顺铂小。另外,与顺铂相比,观察到它们具有同等或更大的细胞毒性活性。