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

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作者
Katarzyna Papierska
Violetta Krajka-Kuźniak
Robert Kleszcz
Tomasz Stefański
Rafał Kurczab
Maciej Kubicki
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[1] Poznan University of Medical Sciences,Department of Pharmaceutical Biochemistry
[2] Adam Mickiewicz University in Poznań,Faculty of Chemistry
[3] Maj Institute of Pharmacology,Department of Medicinal Chemistry
[4] Polish Academy of Sciences,undefined
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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.
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