Öztürk Emine, Subaşı Elif, Kurşunluoğlu Gizem, Yüksel Betül Şen, Kayalı Hülya Ayar
The Graduate School of Natural and Applied Sciences, Dokuz Eylul University, 35100, İzmir, Turkey.
Department of Chemistry, Faculty of Science, Dokuz Eylul University, 35160, İzmir, Turkey.
J Biol Inorg Chem. 2025 Feb;30(1):71-85. doi: 10.1007/s00775-024-02090-w. Epub 2024 Dec 31.
As novel promising anticancer candidates, the piano-stool type complexes of ruthenium, [RuCl(η-p-cymene)(N,S-L)]PF, K-, were synthesized from the reaction of the substituted benzo[b]thiophene based thiosemicarbazone ligands (L) with [{RuCl(η-p-cymene)}(μ-Cl)]. All complexes were fully characterized using elemental analysis, and spectroscopic methods such as FT-IR and H NMR. The molecular masses of the complexes were proved by MALDI-TOF analysis. Single crystal X-ray diffraction study was employed in the structural elucidation of complex K which shows a distorted octahedral geometry around the Ru(II) ion. Furthermore, spectroscopic methods revealed that in all complexes the ligands are coordinated to the metal center in neutral thione form via N, S donors. In this study, the effect of all ligands, complexes and commercial drugs with a different concentration on the viability of OVCAR-3, A2780 and OSE cells were compared. In this comparison, the cytotoxicity of ruthenium (II) complexes on two ovarian cancer cell lines (human A2780 and human OVCAR-3) was evaluated. For this purpose, the resazurin assay was performed. Based on our studies, complex K showed the highest toxicity against OVCAR-3 and A2780 cells. The cytotoxic effect of K was found to be higher than that of the commercial anticancer agents Oxalpin and Carbodex, 1.8-34.7-fold for OVCAR-3 cells and 1.9-11.8-fold for A2780 cells, respectively. These results provide insight into the potential of ruthenium (II) complexes as a cytotoxic agent for the treatment of ovarian cancer, particularly for primary tumors.
作为新型有前景的抗癌候选物,钌的钢琴凳型配合物[RuCl(η-p-异丙基苯)(N,S-L)]PF₆、K⁺,是由基于取代苯并[b]噻吩的硫代氨基脲配体(L)与[{RuCl(η-p-异丙基苯)}(μ-Cl)]反应合成的。所有配合物均通过元素分析以及FT-IR和¹H NMR等光谱方法进行了全面表征。配合物的分子量通过基质辅助激光解吸电离飞行时间(MALDI-TOF)分析得以证实。单晶X射线衍射研究用于配合物K的结构解析,该配合物在Ru(II)离子周围呈现扭曲的八面体几何构型。此外,光谱方法表明,在所有配合物中,配体通过N、S供体以中性硫酮形式与金属中心配位。在本研究中,比较了所有配体、配合物和不同浓度的商业药物对OVCAR-3、A2780和OSE细胞活力的影响。在该比较中,评估了钌(II)配合物对两种卵巢癌细胞系(人A2780和人OVCAR-3)的细胞毒性。为此,进行了刃天青测定。基于我们的研究,配合物K对OVCAR-3和A2780细胞显示出最高的毒性。发现K的细胞毒性作用分别比商业抗癌药物奥沙利铂和卡波地昔高,对OVCAR-3细胞高1.8至34.7倍,对A2780细胞高1.9至11.8倍。这些结果为钌(II)配合物作为治疗卵巢癌,特别是原发性肿瘤的细胞毒性剂的潜力提供了见解。