A5083922003- Metal complexes synthesis and properties
- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Ferrocene Chemistry and Applications
- Lanthanide and Transition Metal Complexes
- Computational Drug Discovery Methods
- Synthesis and biological activity
- Magnetism in coordination complexes
- Synthesis and Characterization of Heterocyclic Compounds
- Cancer therapeutics and mechanisms
- Nanoparticle-Based Drug Delivery
- Protein Interaction Studies and Fluorescence Analysis
- Organometallic Complex Synthesis and Catalysis
- Crystallography and molecular interactions
- Chronic Myeloid Leukemia Treatments
- Click Chemistry and Applications
- Free Radicals and Antioxidants
- Machine Learning in Materials Science
- Analytical chemistry methods development
- Organometallic Compounds Synthesis and Characterization
- Radioactive element chemistry and processing
- Cancer Treatment and Pharmacology
- Nonlinear Optical Materials Research
- Arsenic contamination and mitigation
- Advanced biosensing and bioanalysis techniques
Universität Innsbruck
2023-2025
Trakia University
2023-2024
University of Graz
2018-2023
University of Vienna
2009-2021
Institute of Inorganic Chemistry of the Slovak Academy of Sciences
2021
École Polytechnique Fédérale de Lausanne
2015-2019
Medical University of Sofia
2007-2010
Octahedral platinum(IV) complexes are promising candidates in the fight against cancer. In order to rationalize further development of this class compounds, detailed studies on their mechanisms action, toxicity, and resistance must be provided structure–activity relationships drawn. Herein, we report theoretical QSAR investigations a series 53 novel bis-, tris-, tetrakis(carboxylato)platinum(IV) complexes, synthesized tested for cytotoxicity our laboratories. The hybrid DFT functional wb97x...
A series of six novel bis(carboxylato)dichloridobis(ethylamine)platinum(IV) complexes was synthesized and characterized in detail by elemental analysis, FT-IR, ESI-MS, HPLC, multinuclear (1H, 13C, 15N, 195Pt) NMR spectroscopy one case X-ray diffraction. Cytotoxic properties the were evaluated four human tumor cell lines originating from ovarian carcinoma (CH1 SK-OV-3), colon (SW480) non-small lung cancer (A549) means MTT colorimetrical assay. In addition, their octanol/water partition...
The lipophilic character of novel carboplatin prodrugs was controlled by the choice axial ligand also influencing their cytotoxicity.
A novel class of platinum(IV) complexes the type [Pt(Am)(R(COO)2)2], where Am is a chelating diamine or two monodentate am(m)ine ligands and R(COO)2 dicarboxylato moiety, was synthesized. For this purpose, reaction between corresponding tetrahydroxidoplatinum(IV) precursors various dicarboxylic acids, such as oxalic, malonic, 3-methylmalonic, cyclobutanedicarboxylic acid, utilized. All new compounds were characterized in detail, using 1D 2D NMR techniques, ESI-MS, FTIR spectroscopy,...
Advances in treatment strategies together with an earlier diagnosis have considerably increased the average survival of cancer patients over last four decades. Nevertheless, despite growing number new antineoplastic agents introduced each year, there is still no adequate therapy for problematic malignancies such as pancreatic, lung and stomach cancers. Consequently, it important to ensure that existing drugs used treat other types cancers, potentially diseases, are not overlooked when...
Abstract The selection of drug candidates for entering clinical development relies on in vivo testing (solid) tumor animal models. However, the heterogeneity tissue (e.g. terms uptake or composition) is rarely considered when novel candidates. Therefore, we used murine colon cancer CT-26 model to study spatially-resolved distribution upon repetitive treatment animals over two weeks with three investigational platinum(iv)-based anticancer agents, oxaliplatin satraplatin. A quantitative laser...
A NanoSIMS, LA-ICP-MS and TEM combinatorial approach was applied to analyze the distribution of platinum( iv ) prodrugs in murine tissue samples.
Lipophilicity is a crucial parameter for drug discovery, usually determined by the logarithmic partition coefficient (Log P) between octanol and water. However, available detection methods have restricted widespread use of in inorganic medicinal chemistry, recent investigations shifted towards chromatographic lipophilicity parameters, frequently without conversion to derive Log P. As high-performance liquid chromatography (HPLC) instruments are readily research groups, HPLC-based method...
Oxaliplatin is stable in pure water and DMSO, but reacts rapidly a mixture of the two solvents.
Drug combinations are extensively used to treat cancer and often selected according complementary mechanisms. Here, we describe a cell-based high-throughput screening assay for identification of synergistic between broadly applied platinum-based chemotherapeutics drugs from library composed 1280 chemically pharmacologically diverse (mostly FDA approved) compounds. The was performed on chemoresistant cell lines derived lung (A549) pancreatic (PANC-1) carcinoma, where combination regimens...
Herein, we present a comparative study on the chemistry and biological activity of N-heterocyclic carbene (NHC)Pt(II)/Au(I) complexes. Accordingly, representative compounds cis/trans- [PtL2X2] (X = Cl (5, 6) or I (7, 8)), [PtL3Cl]+ (9), [AuLX] (10) (11)), [AuL2]+ (12) type, where L is 1,3-diethylbenzimidazol-2-ylidene, were synthesized characterized in detail to elucidate role metal center their physicochemical properties. The stability complexes presence cell culture medium reactivity...
Predicting the solubility and lipophilicity of platinum(II, IV) complexes is essential for prioritizing potential anticancer candidates in drug discovery. This study introduces first publicly available online model predicting platinum complexes, addressing lack literature models this regard. Using a time-split dataset, we developed consensus with Root Mean Squared Error (RMSE) 0.62 through 5-cross-validation on training set 284 historical compounds (solubility data reported prior to 2017)....
The reductive biotransformation of platinum( iv ) prodrugs was investigated in whole human blood by HPLC-ICP-MS.
Five new multifunctional Pt(<sc>iv</sc>) prodrugs with a carboplatin core and one or two axial deferoxamine ligands were synthesized. The complexes express multiple effects, including cytotoxicity high affinity towards ferric ions.
Abstract Platinum complexes are a great interest of study, because the antitumor activity and clinical use some them in recent anticancer chemotherapy. In many cases, computational studies can be very useful for predicting structure physicochemical properties metal complexes. Theoretical calculations also used rational design new with optimal ratio: activity/toxicity. The geometry three Pt(II) general formula cis ‐[PtL 2 X ] (where L is 5‐methyl‐5(4‐pyridyl)hydantoin = Cl − , Br I ) free...
(E/Z)-3-(4-((E)-1-(4-Hydroxyphenyl)-2-phenylbut-1-enyl)phenyl)acrylic acid (GW7604) as a carrier was esterified with alkenols of various lengths and coordinated through the ethylene moiety to PtCl3, similar Zeise's salt (K[PtCl3(C2H4)]). The resulting GW7604-Alk-PtCl3 complexes (Alk = Prop, But, Pent, Hex) degraded in aqueous solution only by exchange chlorido ligands. For example, GW7604-Pent-PtCl3 amino alanine cell culture medium, bound isolated nucleotide 5′-GMP, interacted DNA (empty...