Abstract
The oncological use of cisplatin is hindered by its severe side effects and a very important resistance problem. To overcome these problems, scientists have attempted to design new generation transition-metal anticancer complexes. In this study, we present new complexes, ruthenium(II) [(η6-p-cymene)RuCl(py2CO)]PF6 (1), iridium(III) [(η5-Cp)IrCl(py2CO)]PF6 (2), and NH4[IrCl4(py2CO)]·H2O (3), based on di-2-pyridylketone (py2CO). The prepared complexes were characterized by FTIR, 1H, 13C, 15N NMR, UV-Vis, PL and elemental analysis techniques. The single-crystal X-ray structure analysis and comparative data revealed pseudo-octahedral half-sandwich 1 and 2 complexes and octahedral tetrachloroiridate(III) 3 with a rare chelating κ2N,O coordination mode of py2CO. The compounds were tested in vitro against three cancer cell lines—colorectal adenoma (LoVo), myelomonocytic leukaemia (MV-4-11), breast adenocarcinoma (MCF-7), and normal fibroblasts (BALB/3T3). The most promising results were obtained for iridium(III) complex 3 against MV-4-11 (IC50 = 35.8 ± 13.9 µg/mL) without a toxic effect against normal BALB/3T3, which pointed towards its selectivity as a potential anticancer agent. Extensive research into their mode of binding with DNA confirmed for 1 and 2 complexes non-classical binding modes, while the 3D circular dichroism (CD) experiment (ΔTm) suggested that 3 induced the probable formation of covalent bonds with DNA. In addition, the obtained iridium complexes induce ROS, which, in synergy with hydrolysis promoting DNA bonding, may lead to cancer cell death.
Highlights
IntroductionRuthenium and iridium complexes have properties such as a variety of oxidation states of their central ions, tuneable redox properties, a wide range of coordination numbers and a structural diversity modulated by coordinating ligands, which have been widely
Similar to platinum compounds, ruthenium and iridium complexes have properties such as a variety of oxidation states of their central ions, tuneable redox properties, a wide range of coordination numbers and a structural diversity modulated by coordinating ligands, which have been widelyMaterials 2020, 13, 3491; doi:10.3390/ma13163491 www.mdpi.com/journal/materials MaterialsMaterials2020, 13, 3491 x FOR PEER REVIEW2 2ofof coordination numbers and a structural diversity modulated by coordinating ligands, which have studied [1,2]
All the complexes were found to be stable in air and non-hydroscopic
Summary
Ruthenium and iridium complexes have properties such as a variety of oxidation states of their central ions, tuneable redox properties, a wide range of coordination numbers and a structural diversity modulated by coordinating ligands, which have been widely. 2 2ofof coordination numbers and a structural diversity modulated by coordinating ligands, which have studied [1,2]. Such interesting solid-state materials of transition metal complexes have generated been widely studied [1,2]. Most studies on the biological characterization of platinum, ruthenium and iridium have found them to be useful in medicinal chemistry, especially for chemotherapy. This of the of forms of treatment of cancer, which is currently a major
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