A5087288813- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Metal complexes synthesis and properties
- Ferrocene Chemistry and Applications
- Organometallic Complex Synthesis and Catalysis
- Click Chemistry and Applications
- Crystallography and molecular interactions
- Mass Spectrometry Techniques and Applications
- Synthesis and Biological Evaluation
- Analytical chemistry methods development
- Lanthanide and Transition Metal Complexes
- Chemical Synthesis and Analysis
- Trace Elements in Health
- DNA and Nucleic Acid Chemistry
- Synthetic Organic Chemistry Methods
- Protein Interaction Studies and Fluorescence Analysis
- Magnetism in coordination complexes
- Molecular Sensors and Ion Detection
- N-Heterocyclic Carbenes in Organic and Inorganic Chemistry
- Advanced biosensing and bioanalysis techniques
- Synthesis and biological activity
- Supramolecular Chemistry and Complexes
- Metal-Catalyzed Oxygenation Mechanisms
- Organometallic Compounds Synthesis and Characterization
- Radiopharmaceutical Chemistry and Applications
University of Auckland
2016-2025
University of Vienna
2010-2023
Maurice Wilkins Centre
2021-2022
In-Q-Tel
2018
University of Sargodha
2016
Cancer Society of New Zealand
2015
École Polytechnique Fédérale de Lausanne
2007-2014
Translational Research in Oncology
2014
Czech Academy of Sciences, Institute of Inorganic Chemistry
2008-2012
Comprehensive Cancer Center Vienna
2011
This review provides an introduction into the fascinating area of organometallic anticancer compounds. Although subject dates back many years, it has witnessed considerable growth only in past decade. A brief overview together with recent pertinent examples is provided. The properties compounds that lend themselves to medical applications, main current approaches used, and possible avenues for future research are identified.
A series of ruthenium(II)-arene (RAPTA) compounds were evaluated for their ability to inhibit thioredoxin reductase (either cytosolic or mitochondrial) and cathepsin B, two possible targets anticancer metallodrugs. In general, inhibition the reductases was lower than that although selected excellent inhibitors both classes enzymes in comparison other metal-based drugs. Some initial structure-activity relationships could be established. On basis obtained data, different mechanisms...
A phase I and pharmacokinetic study was carried out with the new ruthenium complex indazolium trans-[tetrachlorobis(1H-indazole)ruthenate(III)] (KP1019, FFC14A). Seven patients various types of solid tumours refractory to standard therapy were treated escalating doses KP1019 (25–600 mg) twice weekly for 3 weeks. No dose-limiting toxicity occurred. Ruthenium plasma concentration–time profiles after first dose under multiple-dose conditions analysed using a compartmental approach. The...
The redox properties and GMP-binding of antitumor Ru( iii ) complexes were studied by capillary electrophoresis, NMR spectroscopy square wave voltammetry with regard to the activation such compounds in tumor tissue.
Imidazolium [trans-tetrachloro(1H-imidazole)(S-dimethylsulfoxide)ruthenate(III)] (NAMI-A) and indazolium [trans-tetrachlorobis(1H-indazole)ruthenate(III)] (KP1019) are the most promising ruthenium complexes for anticancer chemotherapy. In this study, azole ligand of NAMI-A was systematically varied (from imidazole to indazole, 1,2,4-triazole, 4-amino-1,2,4-triazole, 1-methyl-1,2,4-triazole), respective were evaluated with regard rate aquation protein binding, redox potentials, cytotoxicity...
Indazolium trans-[tetrachlorobis(1H-indazole)ruthenate(III)] (KP1019) shows particular promise as an antitumour agent against colorectal cancer. It is known that KP1019 reacts with human serum proteins, whereby the major amount binds to albumin (present in large excess) and a smaller transferrin. has been hypothesised transferrin-mediated uptake by transferrin receptor expressing tumour cells may part explain apparent selectivity of this compound. Circular dichroism spectroscopy electrospray...
Water-soluble dinuclear Ru−arene complexes were synthesized and found to exert promising cytotoxic effects in human cancer cells, which could be increased an IC50 of 0.29 μM by increasing the spacer length between metal centers. Cytotoxicity correlated with lipophilicity (log P values) water solubility. The most potent compound, 1,12-bis{chlorido[3-(oxo-κO)-2-methyl-4-pyridinonato-κO4](η6-p-isopropyltoluene)ruthenium}dodecane, is at least 2−3 orders magnitude more active than mononuclear...
Multinuclear platinum anticancer complexes are a proven option to overcome resistance of established compounds. Transferring this concept ruthenium led the synthesis dinuclear Ru(II)−arene compounds containing bis(pyridinone)alkane ligand linker. A pronounced influence spacer length on in vitro activity was found, which is correlated lipophilicity complexes. IC50 values same dimension as for drugs were found human tumor cell lines. No cross-resistance oxoplatin, cisplatin prodrug, observed...
His-tones are not ruth-less: A ruthenium anticancer agent, RAPTA-C, was found to associate with chromatin in cancer cells and form stable, well-defined adducts the nucleosome core at specific histone protein sites (see picture). This illuminates macromolecular binding properties of this antimetastasis agent indicates potential for developing metallodrugs site-selective targeting chromatin.
Despite the severe side effects and emergence of drug resistance, use DNA-targeting platinum drugs remains strong either alone or in a combination chemotherapy regimen. New strategies formulations are being explored design anticancer metal complexes that exhibit nonclassical modes action, selectively hit precise biomolecular targets even able to induce immunogenic activity. These developments will ameliorate systemic toxicity metal-based widen range treatable cancers.