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Analyzing Protein Architectures and Protein-Ligand Complexes by Integrative Structural Mass Spectrometry
Published on: October 15, 2018
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Cyclometalated Gold(III) Complexes Bearing DACH Ligands
Sailajah Gukathasan1, Sean Parkin1, Samuel G Awuah1
1Department of Chemistry , University of Kentucky , Lexington , Kentucky 40506 , United States.
Inorganic Chemistry
|June 29, 2019
Summary
Novel gold(III) complexes with cyclometalated and DACH ligands show promising anticancer activity and selective uptake in cancer cells. These stable compounds offer new insights for designing gold-based anticancer drugs.
Area of Science:
- Inorganic Chemistry
- Medicinal Chemistry
- Chemical Biology
Background:
- Gold(III) complexes are investigated for anticancer properties.
- Cyclometalated ligands and 1,2-diaminocyclohexane (DACH) can stabilize gold(III) complexes.
- Novel scaffolds are needed to explore gold(III) biological activities.
Purpose of the Study:
- Synthesize and characterize novel cyclometalated gold(III) complexes.
- Evaluate the antiproliferative activity and cellular uptake of these complexes.
- Investigate the stability and mechanism of action of the gold(III) compounds.
Main Methods:
- Synthesis and structural characterization of six gold(III) complexes.
- Antiproliferative assays against various cancer cell lines and normal cells.
- DNA interaction studies, cellular uptake measurements, and stability tests.
- Cell cycle analysis to determine the mechanism of action.
Main Results:
- Novel gold(III) complexes of types [Au(C^NH)(DACH)2]+ and [Au(C^N)(DACH)]2+ were synthesized.
- Promising antiproliferative activity with IC50 in the micromolar range and selectivity over normal cells.
- Significant and differential cellular uptake observed in OVCAR8 cancer cells.
- Complexes demonstrated stability under physiological conditions and induced G1 cell cycle arrest.
Conclusions:
- Enhanced Au(III) stabilization by combined cyclometalated and DACH ligands is achievable.
- These novel gold(III) complexes represent a promising scaffold for anticancer drug development.
- Ligand tuning insights can be gained for designing novel gold-based anticancer agents.
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