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2000
Volume 16, Issue 7
  • ISSN: 1871-5206
  • E-ISSN: 1875-5992

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 128;’9.0 to 128;’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.

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/content/journals/acamc/10.2174/1871520616666160201151206
2016-07-01
2025-06-01
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