Recent Advances in Anticancer Activity of Gold(I) Complexes

Area of Science:

• Organometallic chemistry
• Medicinal chemistry
• Oncology

Background:

• Cisplatin's success drives research into new organometallic complexes for cancer treatment.
• Gold complexes, particularly those inhibiting thioredoxin reductase (TrxR), are gaining interest as anticancer agents.
• Auranofin repurposing highlights gold's potential in oncology.

Purpose of the Study:

• To compile and categorize major ligand modifications for gold(I) complexes.
• To evaluate the in vitro anticancer activity of synthesized gold complexes.
• To establish structure-activity relationships for gold(I) anticancer agents.

Main Methods:

• Systematic review and categorization of sulfur-based, nitrogen-containing heterocyclic, carbon-derived, and N-heterocyclic carbene (NHC)-based ligands.
• In vitro evaluation of gold(I) complexes against diverse cancer cell lines.
• Comparative analysis of cytotoxicity data to identify structure-activity relationships.

Main Results:

• Various ligand modifications, including NHC frameworks, extended structural diversity and functional potential.
• Gold(I) complexes demonstrated enhanced biological potential compared to conventional metal complexes.
• Bis-NHC and phosphine-carbon donor ligands showed the most potent anticancer activity, with specific complexes exhibiting submicromolar potency.

Conclusions:

• Rational ligand engineering is critical for enhancing the anticancer efficacy of gold(I) complexes.
• Gold(I) complexes represent a promising class of anticancer agents with potential for targeted drug delivery and multi-mechanistic therapies.
• The study provides a framework for developing next-generation gold-based therapeutics by identifying potent ligand scaffolds.