New IKK inhibitors: Synthesis of new imidazo[1,2-a]quinoxaline derivatives using microwave assistance and biological evaluation as IKK inhibitors
| Autor: | Jean-François Guichou, Pierre-Antoine Bonnet, Georges Moarbess, Olivier Marcadet, Adrien Chouchou, Fiona Leroy, Stéphanie Paniagua-Gayraud, Pierre Cuq, Rémi Ruédas, Carine Deleuze-Masquéfa |
|---|---|
| Rok vydání: | 2016 |
| Předmět: |
0301 basic medicine
Drug Evaluation Preclinical IκB kinase Molecular Docking Simulation 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Quinoxaline Quinoxalines Drug Discovery Binding site Protein Kinase Inhibitors Pharmacology chemistry.chemical_classification Organic Chemistry I-Kappa-B Kinase NF-κB General Medicine I-kappa B Kinase 030104 developmental biology chemistry Biochemistry Docking (molecular) 030220 oncology & carcinogenesis Tricyclic |
| Zdroj: | European Journal of Medicinal Chemistry. 115:268-274 |
| ISSN: | 0223-5234 |
| DOI: | 10.1016/j.ejmech.2016.03.006 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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