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Efficient synthesis and first regioselective C-6 direct arylation of imidazo[2,1-c][1,2,4]triazine scaffold and their evaluation in H2O2-induced oxidative stress.

Authors :
Loubidi, Mohammed
Jouha, Jabrane
Tber, Zahira
Khouili, Mostafa
Suzenet, Franck
Akssira, Mohamed
Erdogan, Mümin Alper
Köse, Fadime Aydın
Dagcı, Taner
Armagan, Güliz
Saso, Luciano
Guillaumet, Gérald
Source :
European Journal of Medicinal Chemistry. Feb2018, Vol. 145, p113-123. 11p.
Publication Year :
2018

Abstract

Oxidative stress and apoptosis are both associated with various acute and chronic disorders. Thus, the aim of the present study is to synthesize imidazo[2,1- c ][1,2,4]triazines derivatives and to evaluate their effects in H 2 O 2 -induced oxidative stress in human neuroblastoma cell line (SH-SY5Y cells). The effects of the compounds on cell viability were measured by MTT assay and the changes in stress and apoptosis-related proteins were investigated by PathScan ® Stress and Apoptosis Signaling Antibody Array kit and Western Blot technique. In particular, four compounds were found to protect SH-SY5Y cells from H 2 O 2 -induced toxicity by increasing Bcl-2/Bax ratio, regulating PI3-K/Akt cascade and inhibiting the ERK pathway. [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
02235234
Volume :
145
Database :
Academic Search Index
Journal :
European Journal of Medicinal Chemistry
Publication Type :
Academic Journal
Accession number :
127672200
Full Text :
https://doi.org/10.1016/j.ejmech.2017.12.081