In recent years, research has found that the cyclooxygenase-2 (COX-2) enzyme is over expressed in cancer cells. Research also indicates that COX-2 inhibition will decrease inflammation associated with tumor growth. Naturally occurring flavonoid compounds, especially aurones, have been shown to effectively inhibit the COX-2 enzyme and subsequently exhibit anti-cancer activity. Mills et. al. previously designed and completed the total synthesis of several novel halogen-substituted aurones. As a continuation of this research, a novel trifluoromethyl substituted aurone has been designed and a synthesis has been proposed. The structure of the COX-2 binding pocket was taken into consideration during design. Increased COX-2 inhibitory activity may be attributed to enhanced steric and electron withdrawing effects from the trifluoromethyl group. The target molecule will be synthesized following the proposed route.

Structure-based design of a novel trifluoromethyl substituted aurone as a potential anticancer agent

243rd National Meeting (2012)

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