Marissa Aubrey, University of North Carolina at Asheville, Asheville, NC and Herman L. Holt Jr., University of North Carolina at Asheville, Asheville, NC.
The ability of chalcones to bind to transition metals is being studied using a variety of nitrogen substituents as ligands on the chalcone backbone. The general structure of the chalcones is synthetically flexible which easily allows for structural modifications. Thus far, a series of chalcones have been synthesized and the formation of nitrogen-containing chalcone ligands is currently underway. Zinc and copper are metals that have been shown to effectively bind to such groups. The metal-chalcone ligand complexes will be identified using spectral and crystallographic methods. By modifying the groups on the chalcone, the water solubility and binding affinity to tubulin can be increased, enhancing the chalcone's cytotoxicity. Ideally, these transition-metal containing molecules will be more water-soluble than previously synthesized chalcones, and demonstrate increased cytotoxicity in cancer cell lines.