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Ruthenium Half-Sandwich Type Complexes with Bidentate Monosaccharide Ligands Show Antineoplastic Activity in Ovarian Cancer Cell Models through Reactive Oxygen Species Production
| Content Provider | MDPI |
|---|---|
| Author | Buglyó, Péter Somsák, László Kacsir, István Sipos, Adrienn Ujlaki, Gyula Bai, Péter Bokor, Éva |
| Copyright Year | 2021 |
| Description | Ruthenium complexes are developed as substitutes for platinum complexes to be used in the chemotherapy of hematological and gynecological malignancies, such as ovarian cancer. We synthesized and screened 14 ruthenium half-sandwich complexes with bidentate monosaccharide ligands in ovarian cancer cell models. Four complexes were cytostatic, but not cytotoxic on A2780 and ID8 cells. The $IC_{50}$ values were in the low micromolar range (the best being 0.87 µM) and were similar to or lower than those of the clinically available platinum complexes. The active complexes were cytostatic in cell models of glioblastoma, breast cancer, and pancreatic adenocarcinoma, while they were not cytostatic on non-transformed human skin fibroblasts. The bioactive ruthenium complexes showed cooperative binding to yet unidentified cellular target(s), and their activity was dependent on reactive oxygen species production. Large hydrophobic protective groups on the hydroxyl groups of the sugar moiety were needed for biological activity. The cytostatic activity of the ruthenium complexes was dependent on reactive species production. Rucaparib, a PARP inhibitor, potentiated the effects of ruthenium complexes. |
| Starting Page | 10454 |
| e-ISSN | 14220067 |
| DOI | 10.3390/ijms221910454 |
| Journal | International Journal of Molecular Sciences |
| Issue Number | 19 |
| Volume Number | 22 |
| Language | English |
| Publisher | MDPI |
| Publisher Date | 2021-09-28 |
| Access Restriction | Open |
| Subject Keyword | International Journal of Molecular Sciences Oncology Ovarian Cancer Ruthenium Complex Half-sandwich Cooperative Binding Reactive Oxygen Species Production Glycosyl Heterocycle Oxadiazole Triazole Rucaparib |
| Content Type | Text |
| Resource Type | Article |
