From previous studies, it is evident that metal-organic gold(I) complexes have antiproliferative activities. The aim of this study is not only to find new anticancer agents but also to overcome existing cytostatic resistance in cancer cells. The synthesis and medicinal evaluation of two cationic 1,3-disubstituted gold(I) bis-tetrazolylidene complexes and are reported. To determine apoptosis-inducing properties of the complexes, DNA fragmentation was measured using propidium iodide staining followed by flow cytometry. Gold(I) complex targets explicitly malignant cells, effectively inhibiting their growth and selectively inducing apoptosis without signs of necrosis. Even in cells resistant to common treatments such as doxorubicin, it overcomes multidrug resistance and sensitizes existing drug-resistant cells to common cytostatic drugs. It is assumed that gold(I) complex involves the mitochondrial pathway in apoptosis and targets members of the BCL-2 family, enhancing its potential as a therapeutic agent in cancer treatment.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC11403678 | PMC |
| http://dx.doi.org/10.1021/acs.jmedchem.4c01117 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Gold(I) N-heterocyclic carbene complexes show strong proapoptotic, antioxidant and anti-inflammatory effects in A2780 and endothelial cells.
Chem Biol Interact
January 2025
Institute of Vascular Biology and Thrombosis Research, Center for Physiology and Pharmacology, Medical University of Vienna, Schwarzspanierstrasse 17, 1090 Vienna, Austria. Electronic address:
A series of eight gold(I) N-heterocyclic carbene (NHC) complexes [Au(IMes)(HLn)] based on 1,3-bis(2,4,6-trimethylphenyl)imidazol-2-ylidene (IMes) and 7-azaindole derivatives (HLn), where n = 1-8 for HL1 = 5-flouro-7-azaindole, HL2 = 5-bromo-7-azaindole, HL3 = 3-chloro-7-azaindole, HL4 = 3-iodo-7-azaindole, HL5 = 5-bromo-3-chloro-7-azaindole, HL6 = 5-bromo-3-iodo-7-azaindole, HL7 = 4-chloro-2-methyl-7-azaindole and HL8 = 7-azaindole, was prepared, characterised and studied for their in vitro anti-cancer and anti-inflammatory effects. The complexes showed significant cytotoxicity on human ovarian cancer cell lines (A2780, IC ≈ 8-19 μM and A2780R, IC ≈ 8-19 μM) and lowered toxicity in normal HaCat and MRC-5 cells. Cellular effects of the selected complexes 1 and 7 were evaluated in A2780 cells using flow cytometry.
View Article and Find Full Text PDFAn Anionic Mesoionic Carbene (anMIC) and its Transformation to Metallo MIC-Boranes: Synthesis and Properties.
Angew Chem Int Ed Engl
January 2025
Freie Universitat Berlin, Chemistry and Biochemistry, Fabeckstraße 34-36, 14195, Berlin, GERMANY.
Neutral mesoionic carbenes (MICs) based on a 1,2,3-triazole core have had a strong impact on various branches of chemistry such as homogeneous catalysis, electrocatalysis, and photochemistry/photophysics. We present here the first general synthesis of anionic mesoionic carbenes (anMICs) based on a 1,2,3-triazole core and a borate backbone. The free anMIC is stable in solution under an inert atmosphere at low temperatures, and can be stored for several weeks.
View Article and Find Full Text PDFNew Gold(I) Complexes as Potential Precursors for Gas-Assisted Methods: Structure, Volatility, Thermal Stability, and Electron Sensitivity.
Molecules
January 2025
Faculty of Chemistry, Nicolaus Copernicus University in Toruń, Gagarina 7, 87-100 Toruń, Poland.
We report the synthesis and characterization of new, user-friendly gold(I) [Au(μ-(NH)CCF)] coordination polymer and [AuCl(NH(NH=)CCF)] complex. These compounds were investigated for potential application as precursors in chemical vapor deposition (CVD) and focused electron/ion beam-induced deposition (FEBID/FIBID), which are additive methods to produce nanomaterials. Single-crystal X-ray diffraction, elemental analysis, and infrared spectroscopy were used to determine the complexes' composition and structure.
View Article and Find Full Text PDFSpecial Issue: "Enzymes and Enzyme Inhibitors-Applications in Medicine and Diagnosis 2.0".
Int J Mol Sci
December 2024
School of Pharmacy, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece.
The first paper in this Special Issue explores the synthesis, characterization, biological, and catalytic activities of new gold(I) and silver(I) complexes that are stabilized by caffeine derivatives and used as NHC ligands [...
View Article and Find Full Text PDFQuinizarin Gold(I) N-Heterocyclic Carbene Complexes with Synergistic Activity Against Anthracycline-Resistant Leukaemia Cells: Synthesis and Biological Activity Studies.
Chemistry
January 2025
Faculty of Chemistry and Biochemistry, Inorganic Chemistry I - Bioinorganic Chemistry, Ruhr University Bochum, Universitaetsstrasse 150, 44801, Bochum, Germany.
Article Synopsis
- New quinizarin-Au(I)-NHC complexes were developed and fully characterized, demonstrating effective growth inhibition in HeLa cervical cancer cells with IC values between 2.4 and 5.3 μM.
- Cytotoxicity studies showed that complex 2 b could overcome anthracycline resistance in K562 leukemia cells and worked synergistically with doxorubicin against both sensitive and resistant leukemia cells.
- The study highlighted that localizing these complexes to mitochondria was crucial for their antiproliferative effects and ability to counteract drug resistance, rather than just overall cytotoxicity.
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!