Fabra David, Mendrina Theresa, Matesanz Ana I, Medrano Ángeles, Pitek Rastislav, Poetsch Isabella, Berger Walter, Heffeter Petra, Quiroga Adoración G
Department of Inorganic Chemistry, School of Sciences, Universidad Autónoma de Madrid (UAM) Madrid 28049 Spain
Center for Cancer Research and Comprehensive Cancer Center, Medical University of Vienna Borschkegasse 8a 1090 Vienna Austria
Inorg Chem Front. 2025 May 12. doi: 10.1039/d5qi00674k.
The design of -platinum(ii) complexes marked a significant turning point in the development of unconventional anticancer metallodrugs. Compared to cisplatin, these complexes induce distinctly different cellular responses and are often active against cisplatin-resistant cell lines. In this study, we synthesized and fully characterized two new Pt(ii) complexes, introducing one acetate (OCOCH) ligand (x) into the -PtXX' axis, where X' is either acetate or chlorido. We evaluated their cytotoxicity across a panel of malignant (Capan-1, B16, MCF7, HCT-116, CT26 and P31) and non-malignant (HaCaT, HUVEC, BEC, and MCF10A) cell lines, finding that the complex with only one acetate to a chlorido group is more active and selective than the complex with two acetates (X = X'). Furthermore, the two complexes differ from cisplatin in their cellular uptake route as well as mode of action by inducing cancer cell death non-DNA-associated mechanisms.
含铂（II）配合物的设计标志着非常规抗癌金属药物研发中的一个重要转折点。与顺铂相比，这些配合物会引发明显不同的细胞反应，并且通常对顺铂耐药的细胞系具有活性。在本研究中，我们合成并全面表征了两种新的铂（II）配合物，在-PtXX'轴中引入了一个乙酸根（OCOCH）配体（x），其中X'为乙酸根或氯离子。我们评估了它们对一系列恶性（Capan-1、B16、MCF7、HCT-116、CT26和P31）和非恶性（HaCaT、HUVEC、BEC和MCF10A）细胞系的细胞毒性，发现含有一个乙酸根与一个氯离子基团的配合物比含有两个乙酸根（X = X'）的配合物更具活性和选择性。此外，这两种配合物在细胞摄取途径以及通过非DNA相关机制诱导癌细胞死亡的作用方式上与顺铂不同。
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