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Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents
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Novel Anticancer NHC*-Gold(I) Complexes Inspired by Lepidiline A
Danielle Curran1, Helge Müller-Bunz1, Sofia I Bär2
1School of Chemistry, University College Dublin, Belfield, Dublin 4, Ireland.
Molecules (Basel, Switzerland)
|August 6, 2020
Summary
New gold(I) N-heterocyclic carbene complexes show potent anticancer activity. Certain compounds demonstrated excellent sub-micromolar efficacy against colon and breast cancer cell lines, highlighting their therapeutic potential.
Area of Science:
- Organometallic Chemistry
- Medicinal Chemistry
- Cancer Research
Background:
- N-Heterocyclic carbene gold(I) complexes (NHC*-Au-L) are investigated as potential anticancer agents.
- Synthesis of novel NHC*-Au-L complexes with varying ligands (L = Br-, I-, C≡C-R, NHC*, PPh3) was performed.
Purpose of the Study:
- To synthesize and characterize novel N-heterocyclic carbene gold(I) complexes.
- To evaluate the in vitro anticancer activity of these complexes against human colon carcinoma (HCT-116wt) and multidrug-resistant breast carcinoma (MCF-7topo) cell lines.
Main Methods:
- Synthesis and X-ray crystallography of gold(I) complexes.
- MTT-based proliferation assays to determine cytotoxicity (IC50 values).
Main Results:
- X-ray structures revealed aurophilic interactions in five complexes.
- Most complexes exhibited cytotoxicity in the low micromolar range.
- Compounds 2c, 3a, and 3b displayed excellent sub-micromolar activity.
Conclusions:
- N-heterocyclic carbene gold(I) complexes are promising anticancer drug candidates.
- Ligand efficacy generally followed the order: carbene > phosphine > alkyne > halide, with notable exceptions.
- Specific complexes show significant potential for further development in cancer therapy.
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