title: New IKK inhibitors: Synthesis of new imidazo[1,2-a]quinoxaline derivatives using microwave assistance and biological evaluation as IKK inhibitors.
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.
authors.affiliation: Lebanese University, Faculty of Sciences II, Department of Chemistry and Biochemistry, Campus Fanar, BP 90656 Jdeideh, Lebanon.
authors.forename: Georges
authors.initials: G
authors.lastname: Moarbess
authors.affiliation: CNRS, UMR5048 - Université de Montpellier, Centre de Biochimie Structurale, F-34090 Montpellier, France; INSERM, U1054, F-34090 Montpellier, France.
authors.forename: Jean-François
authors.initials: JF
authors.lastname: Guichou
authors.affiliation: Institut des Biomolécules Max Mousseron (IBMM), UMR 5247, CNRS, Université Montpellier, ENSCM, Faculté de Pharmacie, 15, avenue Charles Flahault,BP14491, 34093 Montpellier cedex 5, France.
authors.forename: Stéphanie
authors.initials: S
authors.lastname: Paniagua-Gayraud
authors.affiliation: Institut des Biomolécules Max Mousseron (IBMM), UMR 5247, CNRS, Université Montpellier, ENSCM, Faculté de Pharmacie, 15, avenue Charles Flahault,BP14491, 34093 Montpellier cedex 5, France.
authors.forename: Adrien
authors.initials: A
authors.lastname: Chouchou
authors.affiliation: Institut des Biomolécules Max Mousseron (IBMM), UMR 5247, CNRS, Université Montpellier, ENSCM, Faculté de Pharmacie, 15, avenue Charles Flahault,BP14491, 34093 Montpellier cedex 5, France.
authors.forename: Olivier
authors.initials: O
authors.lastname: Marcadet
authors.affiliation: Institut des Biomolécules Max Mousseron (IBMM), UMR 5247, CNRS, Université Montpellier, ENSCM, Faculté de Pharmacie, 15, avenue Charles Flahault,BP14491, 34093 Montpellier cedex 5, France.
authors.forename: Fiona
authors.initials: F
authors.lastname: Leroy
authors.affiliation: Institut des Biomolécules Max Mousseron (IBMM), UMR 5247, CNRS, Université Montpellier, ENSCM, Faculté de Pharmacie, 15, avenue Charles Flahault,BP14491, 34093 Montpellier cedex 5, France.
authors.forename: Rémi
authors.initials: R
authors.lastname: Ruédas
authors.affiliation: Institut des Biomolécules Max Mousseron (IBMM), UMR 5247, CNRS, Université Montpellier, ENSCM, Faculté de Pharmacie, 15, avenue Charles Flahault,BP14491, 34093 Montpellier cedex 5, France.
authors.forename: Pierre
authors.initials: P
authors.lastname: Cuq
authors.affiliation: Institut des Biomolécules Max Mousseron (IBMM), UMR 5247, CNRS, Université Montpellier, ENSCM, Faculté de Pharmacie, 15, avenue Charles Flahault,BP14491, 34093 Montpellier cedex 5, France. Electronic address: carine.masquefa@umontpellier.fr.
authors.forename: Carine
authors.initials: C
authors.lastname: Deleuze-Masquéfa
authors.affiliation: Institut des Biomolécules Max Mousseron (IBMM), UMR 5247, CNRS, Université Montpellier, ENSCM, Faculté de Pharmacie, 15, avenue Charles Flahault,BP14491, 34093 Montpellier cedex 5, France.
authors.forename: Pierre-Antoine
authors.initials: PA
authors.lastname: Bonnet
mesh_terms: D004353:Drug Evaluation, Preclinical; D051550:I-kappa B Kinase / Q000037:antagonists & inhibitors*; D062105:Molecular Docking Simulation; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011810:Quinoxalines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D047428:Protein Kinase Inhibitors; D011810:Quinoxalines; D051550:I-kappa B Kinase
keywords: IKK inhibitors; Imidazoquinoxalines; NF-κB