Enhancing the anti-inflammatory activity of chalcones by tuning the Michael acceptor site.

@article{Rcker2015EnhancingTA,
  title={Enhancing the anti-inflammatory activity of chalcones by tuning the Michael acceptor site.},
  author={Hannelore R{\"u}cker and Nafisah Al-Rifai and Anne Rascle and Eva Gottfried and Lidia Brodziak-Jarosz and Clarissa Gerh{\"a}user and Tobias P Dick and Sabine Amslinger},
  journal={Organic & biomolecular chemistry},
  year={2015},
  volume={13 10},
  pages={3040-7}
}
Inflammatory signaling pathways orchestrate the cellular response to infection and injury. These pathways are known to be modulated by compounds that alkylate cysteinyl thiols. One class of phytochemicals with strong thiol alkylating activity is the chalcones. In this study we tested fourteen chalcone derivatives, α-X-substituted 2',3,4,4'-tetramethoxychalcones (α-X-TMCs, X = H, F, Cl, Br, I, CN, Me, p-NO2-C6H4, Ph, p-OMe-C6H4, NO2, CF3, COOEt, COOH), for their ability to modulate inflammatory… CONTINUE READING