Design, Synthesis, and Biological Activity of Coniferyl Aldehyde Derivatives as Potential Anticancer and Antioxidant Agents

Abstract

Natural products are known to exhibit antimicrobial, anticancer, and antioxidant activities. Among these natural products is cinnamon which contains cinnamaldehyde. Cinnamaldehyde and its derivatives have been reported to have anticancer and antioxidant activities. Coniferyl aldehyde, a non-cytotoxic compound and a cinnamaldehyde derivative, has also been shown to have anticancer activity. In this study, several derivatives of coniferyl aldehyde were synthesized and evaluated for their anticancer and antioxidant activities. Compounds 1, 2, 4, and 8-11 showed cytotoxic activity against H1299 cell line, a non-small cell lung cancer cells, with 4 being the most potent with IC50 value of 6.7 μM. The antioxidant assay experiment showed that compounds 1, 2, and 4 resulted in half the scavenging activity of vitamin C at all tested concentrations. The coniferyl aldehyde itself showed dose-dependent antioxidant activity, with a proposed free radical stabilization mechanism. Thus, our study showed that the synthesized coniferyl aldehyde derivatives exhibit anticancer and antioxidant activities, which might act as potential therapeutic agents.