This project aims to design new anticancer drugs by using N-heterocyclic carbenes (NHC), gold (Au), and selenium (Se), which have not been explored before.
NHCs are chosen as key ligands in homogeneous catalysis with transition metals. Gold compounds, like auranofin, disrupt tumor growth by inhibiting key enzymes. Se triggers cancer cell death by inducing oxidative stress and blocking sulfur-based cell components.
Cancer poses a global threat, causing millions of deaths and huge economic losses, while available chemotherapy often leads to severe side effects and drug resistance. Therefore, there is a need for more effective and less toxic drugs. I synthesized and tested several drug candidates in in vitro cancer models, showing selective anticancer activity superior to cisplatin.
The project uses a "weak base route" to synthesize these new compounds, following green chemistry principles to reduce the ecological impact of chemical synthesis. The proposed synthetic strategy uses non-toxic solvents and energy-saving protocols to promote sustainable drug development.
Cell-free and cell-based assays will assess cytotoxicity, efficacy, and selectivity towards the TrxR1 enzyme, which is critical to cancer growth. Molecular docking will confirm the inhibition of the biological target, allowing structure-activity relationship (SAR) analysis to optimize drug structure. By refining the NHC ligand, Au-Se linker, and low core scaffold, the project aims to develop highly effective, targeted anticancer drugs.
This research seeks to advance cancer treatment by creating targeted drugs that reduce side effects and improve patient outcomes. Additionally, it aligns with the EU's sustainability goals, promoting environmentally responsible drug development. The project also strengthens European cooperation in cancer research, both in academia and industry, and will inspire future chemists, with broader economic benefits through innovation in healthcare.