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

被引：17

作者：

Moarbess, Georges ^{[1
]}

Guichou, Jean-Francois ^{[2
,3
]}

Paniagua-Gayraud, Stephanie ^{[4
]}

Chouchou, Adrien ^{[4
]}

Marcadet, Olivier ^{[4
]}

Leroy, Fiona ^{[4
]}

Ruedas, Remi ^{[4
]}

Cuq, Pierre ^{[4
]}

Deleuze-Masquefa, Carine ^{[4
]}

Bonnet, Pierre-Antoine ^{[4
]}

机构：

[1] Lebanese Univ, Fac Sci 2, Dept Chem & Biochem, Campus Fanar,BP 90656, Jdeideh, Lebanon

[2] Univ Montpellier, CNRS, UMR5048, Ctr Biochim Struct, F-34090 Montpellier, France

[3] INSERM, U1054, F-34090 Montpellier, France

[4] Univ Montpellier, CNRS, IBMM, UMR 5247,ENSCM,Fac Pharm, 15 Ave Charles Flahault,BP14491, F-34093 Montpellier 5, France

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2016年 / 115卷

关键词：

Imidazoquinoxalines; IKK inhibitors; NF-kappa B; NF-KAPPA-B; KINASE-BETA; IN-VITRO; ALPHA; PHOSPHORYLATION; ACTIVATION; PATHWAY; CELLS; UBIQUITINATION; INFLAMMATION;

D O I：

10.1016/j.ejmech.2016.03.006

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The inhibition of the NF-kappa B-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. (C) 2016 Elsevier Masson SAS. All rights reserved.

引用

页码：268 / 274

页数：7

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