Organometallic ruthenium complex of quinolone antibacterial agent ofloxacin was isolated and its crystal structure was determined. In this »piano-stool« complex, quinolone is bidentately coordinated to the metal through the ring carbonyl and one of the carboxylic oxygen atoms. Interactions of the title complex with DNA were studied by spectroscopic methods (electronic, fluorescence, CD) and atomic force microscopy (AFM). Preliminary biological tests have also been performed.
The triazole ligand prepared by click chemistry was investigated as novel chelating ligand for Ru(II) complexes with potential antitumor activity. The preparation and structural characterization of four new Ru(II) complexes was performed. In all compounds triazole binds to ruthenium in a bidentate fashion through the pyridyl nitrogen atom and the triazole N2. Selected compounds were tested also in vitro for cytotoxic activity against two human cancer cell lines. It was found that one compound was more cytotoxic than cisplatin against human lung squamose carcinoma cell line (A-549).
In our study, the ruthenium-based anticancer agent KP1339 was tested in combination with electroporation for its cytotoxic effect on CHO and SA-1 cell lines in vitro and on SA-1 murine tumour model in vivo. Our results show that electroporation does not potentiate the cytotoxicity of KP1339 in vitro, but significantly potentiates antitumour effectiveness in vivo. The observed antitumour effectiveness is the result of both the direct cytotoxicity of KP1339 and an antivascular effect of electroporation.
Novel ruthenium(III) complexes with histamine [RuCl4(dmso-S)(histamineH)]•H2O (1a) and [RuCl4(dmso-S)(histamineH)] (1b) have been prepared and characterized by X-ray structure analysis. Their crystal structures are similar and show a protonated amino group on the side chain of the ligand which is not very common for a simple heterocyclic derivative such as histamine. Biological assays to test the cytotoxicity of the compound 1b combined with electroporation were performed to determine its potential for future medical applications in cancer treatment.
Novel compound, (acvH)[trans-RuCl4(dmso-O)NO] (dmso-O is dimethylsulfoxide coordinated through oxygen atom), was isolated from the reaction between antiviral drug acyclovir (acv) and ruthenium precursor ((dmso)2H)[trans-RuCl4(dmso-O)NO]. Crystal structure revealed that compound is of ionic type, containing N(7) protonated acyclovir (acvH) which is not coordinated to the metal center. There is a distorted octahedral coordination around ruthenium(II) center in novel compound.