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<p>As novel promising anticancer candidates, the piano-stool type complexes of ruthenium, [RuCl(η<sup>6</sup>-<i>p</i>-cymene)(<i>N,S</i>-L<sub>n</sub>)]PF<sub>6</sub>, <b>K</b><sub><b>1</b></sub><b>-</b><sub><b>4</b></sub>, were synthesized from the reaction of the substituted benzo[b]thiophene based thiosemicarbazone ligands (L<sub>1-4</sub>) with [{RuCl(η<sup>6</sup>-<i>p</i>-cymene)}<sub>2</sub>(μ-Cl)<sub>2</sub>]. All complexes were fully characterized using elemental analysis, and spectroscopic methods such as FT-IR and <sup>1</sup>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 <b>K</b><sub><b>1</b></sub> 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<sub><b>2</b></sub> showed the highest toxicity against OVCAR-3 and A2780 cells. The cytotoxic effect of K<sub><b>2</b></sub> 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.</p> Graphical Abstract <p></p>

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Anticancer potential of benzo[b]thiophene functionalized thiosemicarbazone ligands and their organoruthenium complexes

  • 期刊论文

  • 发表日期：

    2024年12月31日

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  • Emine Öztürk,
  • Elif Subaşı,
  • Gizem Kurşunluoğlu,
  • Betül Şen Yüksel,
  • Hülya Ayar Kayalı

摘要

As novel promising anticancer candidates, the piano-stool type complexes of ruthenium, [RuCl(η6-p-cymene)(N,S-Ln)]PF6, K1-4, were synthesized from the reaction of the substituted benzo[b]thiophene based thiosemicarbazone ligands (L1-4) with [{RuCl(η6-p-cymene)}2(μ-Cl)2]. All complexes were fully characterized using elemental analysis, and spectroscopic methods such as FT-IR and 1H 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 K1 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 K2 showed the highest toxicity against OVCAR-3 and A2780 cells. The cytotoxic effect of K2 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.

Graphical Abstract