The two independent and coordination sites of a newly synthesized bis[2‐(hydroxyphenyl)‐1,2,4‐triazole] platform have been exploited to prepare four monometallic neutral ()Pt^II complexes carrying DMSO, pyridine, triphenylphosphine, or N‐heterocyclic carbene as the fourth ligand. Then, the second coordination site was used to introduce an IR‐active rhenium tricarbonyl entity, affording the four corresponding heterobimetallic neutral Pt^II/Re^I complexes, as well as a cationic Pt^II/Re^I derivative. X‐ray crystallographic studies showed that distortion of the organic platform occurred to accommodate the coordination geometry of both metal centers. No ligand exchange or transchelation occurred upon incubation of the Pt^II complexes in aqueous environment or in the presence of Fe^III, respectively. The antiproliferative activity of the ligand and complexes was first screened on the triple‐negative breast cancer cell line MDA‐MB‐231. Then, the IC₅₀ values of the most active candidates were determined on a wider panel of human cancer cells (MDA‐MB‐231, MCF‐7, and A2780), as well as on a nontumorigenic cell line (MCF‐10A). Low micromolar activities were reached for the complexes carrying a DMSO ligand, making them the first examples of highly active, but hydrolytically stable, Pt^II complexes. Finally, the characteristic mid‐IR signature of the {Re(CO)₃} fragment in the Pt/Re heterobimetallic complexes was used to quantify their uptake in breast cancer cells.

中文翻译：

---

一种双螯合的^ O / NN ^配体，用于合成异双金属铂（II）/ hen（I）配合物：用于优化新型铂（II）抗癌剂的工具。

利用新合成的双[2-（羟基苯基）-1,2,4-三唑]平台的两个独立且协调的位点来制备四种带有DMSO，吡啶，三苯基膦或N-的单金属中性（）Pt ^II配合物杂环卡宾作为第四配体。然后，第二个配位位点用于引入具有IR活性的三羰基rh实体，提供了四个相应的异双金属中性Pt ^II / Re ^I络合物以及阳离子Pt ^II / Re ^I衍生物。X射线晶体学研究表明，有机平台发生了变形，以适应两个金属中心的配位几何形状。在水性环境中或在Fe ^III的存在下孵育Pt ^II复合物时，未发生配体交换或螯合转移。首先在三阴性乳腺癌细胞系MDA-MB-231上筛选了配体和复合物的抗增殖活性。然后，IC ₅₀在更广泛的人类癌细胞（MDA-MB-231，MCF-7和A2780）以及非致瘤细胞系（MCF-10A）上确定最活跃的候选基因的值。带有DMSO配体的配合物的微摩尔活性较低，使其成为高活性但水解稳定的Pt ^II配合物的第一个实例。最后，将Pt / Re异双金属配合物中{Re（CO）₃ }片段的特征性IR中间特征用于量化其在乳腺癌细胞中的摄取。