Title:Synthesis of 4-piperidone Based Curcuminoids with Anti-inflammatory and Anti-Proliferation Potential in Human Cancer Cell Lines
Volume: 16
Issue: 7
Author(s): Amit Anthwal, Kundan Singh, M. S.M. Rawat, Amit K. Tyagi, Ashanul Haque, Imran Ali and Diwan S. Rawat
Affiliation:
Keywords:
Anti-inflammatory, anti-proliferation, chronic myeloid leukemia, curcumin, colon cancer, cytotoxicity.
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)-α-induced nuclear factor (NF)-κB. All
compounds, except one, were found to exhibit better cytotoxicity than curcumin at 5 μM.
Furthermore, many compounds have shown good potential to inhibit the TNF-α-induced NF-κB activation. Docking study of the
compounds with NF-κB 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-κB where polynucleotides are
known to bind to exhibit their activity.
