| Literature DB >> 27017554 |
Georges Moarbess1, Jean-François Guichou2, Stéphanie Paniagua-Gayraud3, Adrien Chouchou3, Olivier Marcadet3, Fiona Leroy3, Rémi Ruédas3, Pierre Cuq3, Carine Deleuze-Masquéfa4, Pierre-Antoine Bonnet3.
Abstract
The inhibition of the NF-κB-dependent pathways by IKK inhibitors plays an important role in immunity, inflammation, and cancer. New imidazoquinoxalines tricyclic derivatives are prepared using microwave assistance and their biological activities as IKK inhibitors are described. Compounds 6a present a potent inhibition activity and selectivity for IKK2. Docking studies in the IKK2 binding site allowed identification of residues most likely to interact with theses inhibitors and explain their potent IKK2 inhibition activity and selectivity.Entities:
Keywords: IKK inhibitors; Imidazoquinoxalines; NF-κB
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Year: 2016 PMID: 27017554 DOI: 10.1016/j.ejmech.2016.03.006
Source DB: PubMed Journal: Eur J Med Chem ISSN: 0223-5234 Impact factor: 6.514