The synthesis of novel thioderivative chalcones and their influence on NF-κB, STAT3 and NRF2 signaling pathways in colorectal cancer cells

Sci Rep. 2022 Sep 1;12(1):14915. doi: 10.1038/s41598-022-18981-4.

Abstract

This study aimed to synthesize new thioderivative chalcones and analyze their impact on the NF-κB, STAT3, EGFR and Nrf2 signaling pathways in colorectal cancer cells. Among the studied compounds, derivatives 4 and 5 decreased the activation of NF-κB and the expression of the target gene COX-2. In the case of STAT3, we observed the inhibition of activation of this signaling pathway after influencing derivative 4. Increased activation of the Nrf2 signaling pathway was demonstrated for derivatives 5 and 7 in DLD-1 and HCT116 cells. The results of this study indicated that new chalcone derivatives, especially compounds 4, 5, and-to some degree-7, possess potential applications in the prevention of colorectal cancer.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Chalcone* / chemistry
  • Chalcones* / chemistry
  • Chalcones* / pharmacology
  • Colorectal Neoplasms* / drug therapy
  • Colorectal Neoplasms* / metabolism
  • Humans
  • NF-E2-Related Factor 2 / drug effects
  • NF-E2-Related Factor 2 / metabolism
  • NF-kappa B / drug effects
  • NF-kappa B / metabolism
  • STAT3 Transcription Factor / drug effects
  • STAT3 Transcription Factor / metabolism
  • Signal Transduction* / drug effects

Substances

  • Chalcone
  • Chalcones
  • NF-E2-Related Factor 2
  • NF-kappa B
  • STAT3 protein, human
  • STAT3 Transcription Factor