Synthesis of novel halogen substituted aurones as potential anticancer agents

CHED 1323

Kevin F. Dunn, kevin_dunn@ecats.gcsu.edu, Gavin H. Denmark, gavin_denmark@ecats.gcsu.edu, and Chavonda J. Mills, chavonda.mills@gcsu.edu. Department of Chemistry and Physics, Georgia College & State University, 231 W. Hancock Street, Campus Box 82, Milledgeville, GA 31061
Naturally occurring flavonoid compounds have shown great biological potential in recent years, in particular the subclass of flavonoids known as aurones. Previous studies have shown that aurones exhibit anti-cancer activity as well as a variety of other pharmacological activities, including anti-inflammatory and anti-viral properties. More specifically, these studies indicate that aurones show potential in inhibiting cyclooxygenase-2 activity (COX-2), which plays an integral part in inflammation and its associated diseases, such as cancer. Furthermore, structure-activity studies have shown that halogen substituents increase anti-cancer activities of flavonoid derivatives. Therefore, the evaluation of “A” ring halogen substituted aurones is of great importance. As a result, a series of halogen substituted aurones were synthesized and characterized through NMR, IR, and elemental analysis. The synthetic methods used proved successful in the synthesis of the desired halogen substituted aurones.