通过对苯二醛和 2'-羟基苯乙酮的羟醛缩合合成了双(查尔酮)分子 (H2L)，并将其用作桥配体，用于制备组成为 [Cu(NN)(μ-) 的五种双核铜 (II) 配合物。 L)Cu(NN)](NO3)2⋅nH2O (n = 0-2) (1-5)，其中 NN 代表二齿 N 供体配体，例如 phen (1,10-菲咯啉, 1)、bpy (2,2'-联吡啶，2)、mebpy (5,5'-二甲基-2,2'-联吡啶，3)、bphen（红菲咯啉，4）和 nphen（5-硝基-1,10-菲咯啉，5） ）。通过不同的合适技术对化合物进行表征，以确认其纯度、组成和结构。此外，还评估了这些产品对一组人类癌细胞系的体外细胞毒性：卵巢癌细胞系（A2780）、顺铂耐药的卵巢癌细胞系（A2780R）、前列腺癌细胞系（PC3）、骨肉瘤细胞系（HOS）、乳腺癌细胞系（MCF7）和肺癌细胞系（A2780R）。 A549) 和正常成纤维细胞 (MRC-5)，在大多数情况下表现出显着的细胞毒性，IC50 ≈ 0.35-7.8 μM。此外，还进行了时间依赖性细胞毒性和铜的细胞摄取，以及关于细胞周期停滞、诱导细胞死亡和自噬以及诱导 A2780 细胞中细胞内 ROS/超氧化物产生的流式细胞术研究。 A2780细胞的生物学测试结果指出了一种可能的作用机制，其特征是通过触发与线粒体结构损伤和线粒体膜电位耗竭相关的内在信号通路，使G2/M细胞周期停滞并诱导细胞凋亡。概要：带有桥联双（查耳酮）配体的双核 Cu(II) 配合物显示出高体外细胞毒性，引发 A2780 细胞停滞在 G2/M 期，并有效触发细胞凋亡的内在途径。版权所有 © 2024 Elsevier Inc. 保留所有权利。

A bis(chalcone) molecule (H2L) was synthesized via Aldol's condensation from terephthalaldehyde and 2'-hydroxyacetophenone and it was used as bridging ligand for the preparation of five dinuclear copper(II) complexes of the composition [Cu(NN)(μ-L)Cu(NN)](NO3)2⋅nH2O (n = 0-2) (1-5), where NN stands for a bidentate N-donor ligand such as phen (1,10-phenanthroline, 1), bpy (2,2'-bipyridine, 2), mebpy (5,5'-dimethyl-2,2'-dipyridine, 3), bphen (bathophenanthroline, 4) and nphen (5-nitro-1,10-phenanthroline, 5). The compounds were characterized by different suitable techniques to confirm their purity, composition, and structure. Moreover, the products were evaluated for their in vitro cytotoxicity on a panel of human cancer cell lines: ovarian (A2780), ovarian resistant to cisplatin (A2780R), prostate (PC3), osteosarcoma (HOS), breast (MCF7) and lung (A549), and normal fibroblasts (MRC-5), showing significant cytotoxicity in most cases, with IC50 ≈ 0.35-7.8 μM. Additionally, the time-dependent cytotoxicity and cellular uptake of copper, together with flow cytometric studies concerning cell-cycle arrest, induction of cell death and autophagy and induction of intracellular ROS/superoxide production in A2780 cells, were also performed. The results of biological testing on A2780 cells pointed out a possible mechanism of action characterized by the G2/M cell cycle arrest and induction of apoptosis by triggering the intrinsic signalling pathway associated with the damage of mitochondrial structure and depletion of mitochondrial membrane potential. SYNOPSIS: Dinuclear Cu(II) complexes bearing a bridging bis(chalcone) ligand revealed high in vitro cytotoxicity, initiated A2780 cell arrest at G2/M phase and efficiently triggered intrinsic pathway of apoptosis.Copyright © 2024 Elsevier Inc. All rights reserved.