Abstract
A series of 4-piperidone based curcuminoids were synthesized and anticancer potential of these compounds was evaluated against human myeloid leukemia (KBM5) and colon cancer (HCT116) cell lines. Their anti-inflammatory potential was determined through the down-regulation of tumor necrosis factor (TNF)-alpha-induced nuclear factor (NF)-kappa B. All compounds, except one, were found to exhibit better cytotoxicity than curcumin at 5 mu M. Furthermore, many compounds have shown good potential to inhibit the TNF-alpha-induced NF-kappa B activation. Docking study of the compounds with NF-kappa B revealed that the binding affinity of the compounds ranged from -9.0 to -6.5 kcal/mol with 0-8 H-bonds. It was also observed that amido-ether based mono-carbonyl compounds bound around the same region of NF-kappa B where polynucleotides are known to bind to exhibit their activity.