Literature DB >> 27017554

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

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.
Copyright © 2016 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  IKK inhibitors; Imidazoquinoxalines; NF-κB

Mesh:

Substances:

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


  3 in total

Review 1.  Recent advances in the transition-metal-free synthesis of quinoxalines.

Authors:  Biplob Borah; L Raju Chowhan
Journal:  RSC Adv       Date:  2021-11-19       Impact factor: 4.036

2.  Development of (4-Phenylamino)quinazoline Alkylthiourea Derivatives as Novel NF-κB Inhibitors.

Authors:  Sarah S Darwish; Po-Jen Chen; Mostafa M Hamed; Reem A Wagdy; Shun-Hua Chen; Ashraf H Abadi; Mohammad Abdel-Halim; Tsong-Long Hwang; Matthias Engel
Journal:  Pharmaceuticals (Basel)       Date:  2022-06-22

3.  Design and Synthesis of Non-Covalent Imidazo[1,2-a]quinoxaline-Based Inhibitors of EGFR and Their Anti-Cancer Assessment.

Authors:  Manvendra Kumar; Gaurav Joshi; Sahil Arora; Tashvinder Singh; Sajal Biswas; Nisha Sharma; Zahid Rafiq Bhat; Kulbhushan Tikoo; Sandeep Singh; Raj Kumar
Journal:  Molecules       Date:  2021-03-09       Impact factor: 4.411

  3 in total

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