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


Loubıdı M., Jouha J., Tber Z., Khouılı M., Suzenet F., Akssıra M., ...Daha Fazla

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, cilt.145, ss.113-123, 2018 (SCI İndekslerine Giren Dergi) identifier identifier identifier

  • Cilt numarası: 145
  • Basım Tarihi: 2018
  • Doi Numarası: 10.1016/j.ejmech.2017.12.081
  • Dergi Adı: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
  • Sayfa Sayıları: ss.113-123

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.