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

Makaleler > Tam Makale · 2017

Yazarlar: Mohammed Loubıdı, Jabrane Jouha, Zahira Tber, Mostafa Khouılı, Franck Suzenet, Mohamed Akssıra, Mumin Alper Erdogan, FADİME AYDIN KÖSE, Taner DAĞCI, Güliz ARMAGAN, Luciano Saso, Gerald Guıllaumet

European Journal of Medicinal Chemistry, SCI Expanded İndekslerine Giren Dergi, Uluslararası, Wos, 2017, cilt 145, ss 113-123

DOI: 10.1016/j.ejmech.2017.12.081

Özet

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 H2O2-induced oxidative stress in human neuroblastoma cell line (SH-SY5Y cells). The effects of the compounds on cell viability were measured by MIT assay and the changes in stress and apoptosis-related proteins, were investigated by PathScae (R) Stress and Apoptosis Signaling Antibody Array kit and Western Blot technique. In particular, four compounds were found to protect SH-SY5Y cells from H2O2 induced toxicity by increasing Bcl-2/Bax ratio, regulating PI3-K/Alct cascade and inhibiting the ERK pathway. (C) 2017 Published by Elsevier Masson SAS.

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