Synthesis of 4-piperidone Based Curcuminoids with Anti-inflammatory and Anti-Proliferation Potential in Human Cancer Cell Lines

Author(s): Amit Anthwal , Kundan Singh , M. S.M. Rawat , Amit K. Tyagi , Ashanul Haque , Imran Ali , Diwan S. Rawat .

Journal Name: Anti-Cancer Agents in Medicinal Chemistry

Volume 16 , Issue 7 , 2016

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Graphical 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.

Keywords: Anti-inflammatory, anti-proliferation, chronic myeloid leukemia, curcumin, colon cancer, cytotoxicity.

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Article Details

Year: 2016
Page: [841 - 851]
Pages: 11
DOI: 10.2174/1871520616666160201151206
Price: $58

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