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Eur J Med Chem. 2016 Jun 10;115:268-74. doi: 10.1016/j.ejmech.2016.03.006. Epub 2016 Mar 17.

New IKK inhibitors: Synthesis of new imidazo[1,2-a]quinoxaline derivatives using microwave assistance and biological evaluation as IKK inhibitors.

Author information

1
Lebanese University, Faculty of Sciences II, Department of Chemistry and Biochemistry, Campus Fanar, BP 90656 Jdeideh, Lebanon.
2
CNRS, UMR5048 - Université de Montpellier, Centre de Biochimie Structurale, F-34090 Montpellier, France; INSERM, U1054, F-34090 Montpellier, France.
3
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.
4
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.

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.

KEYWORDS:

IKK inhibitors; Imidazoquinoxalines; NF-κB

PMID:
27017554
DOI:
10.1016/j.ejmech.2016.03.006
[Indexed for MEDLINE]

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