简介：钌(II)配合物最近已成为抗癌治疗的候选者，其活性与亲脂性、细胞定位以及与生物分子的特异性相互作用有关。方法：在这项工作中，基于 [Ru(phen)2(dipyrido[3,2-f:2',3'-h]quinoxaline]2 框架合成并报道了两种新型配合物。结果：与母体复合物中，环戊烯和环己烯环与延伸配体的退火显着增加了对许多癌细胞系的细胞毒性，并诱导细胞凋亡。该复合物定位于癌细胞的细胞核中，并与 DNA 上的 DAPI 共定位。DNA 结合研究表明两种复合物都与 DNA 牢固结合，一种复合物像母体一样插入 DNA，而另一种似乎具有多种相互作用模式。讨论：新型复合物增加的亲脂性很可能是增加其细胞毒性的关键因素，而不是比其 DNA 结合模式。版权所有 © 2023 Nyong-Bassey、Hicks、Bergin、Tuite、Kozhevnikov 和 Veuger。

Introduction: Ruthenium(II) complexes have emerged recently as candidates for anti-cancer therapy, where activity is related to lipohilicity, cellular localization, and specific interactions with biomolecules. Methods: In this work, two novel complexes were synthesized and are reported based on the [Ru(phen)2(dipyrido[3,2-f:2',3'-h]quinoxaline]2+ framework. Results: Compared to the parent complex, annealing of cyclopenteno and cyclohexeno rings to the extended ligand substantially increased cytotoxicity towards a number of cancer cell lines, and induced apoptosis. The complexes localize in the nuclei of cancer cells and co-locate with DAPI on DNA. DNA binding studies show that both complexes bind strongly to DNA and one complex intercalates DNA like the parent, whilst the other appears to have multiple modes of interaction. Discussion: It is likely that the increased lipophilicity of the novel complexes is a key factor for increasing their cytotoxicity, rather than their DNA binding mode.Copyright © 2023 Nyong-Bassey, Hicks, Bergin, Tuite, Kozhevnikov and Veuger.