Recently, organometallic compounds have gained in importance in the research of anti-tumor agents. These also include representatives of iridium and osmium. In this work we presented the preaparation of a series of cationic chlorido arene-iridium(III) and arene-osmium(II) complexes with bidentate pyridyl functionalized mesoionic carbenes (MIC) of the 1,2,3-triazol-5-ylidene type. Five complexes have been characterized by X-ray structural analysis. All complexes have been studied for their cytotoxic activity on a human cervical carcinoma HeLa cell line, showing IC50 values up to 2.01 µM. Examination of their cytotoxic effect on different cell lines revealed that they preferentially kill cancer over normal cells. The two most ccytotoxic compounds arrested cells in G2 and induced a dose-dependent increase in SubG0/G1 cell population. Apoptosis, as the primary mode of cell death, was confirmed by Annexin V/PI staining, detection of cleaved PARP, and caspases 3 and 7 activity upon treatment of HeLa cells with both compounds. The role of glutathione (GSH) in the protection of cells against cytotoxicity was confirmed by pretreatment of cells either with buthionine sulfoximine (inhibitor of GSH synthesis) or N-acetyl-cysteine (precursor in GSH synthesis). Project leader Aljoša Bolje contributed as the first author for the publication in collaboration with an international team of researchers.
COBISS.SI-ID: 1538414787