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

Autor: Guliz Armagan, Taner Dagci, Jabrane Jouha, Gérald Guillaumet, Zahira Tber, Mohammed Loubidi, Mostafa Khouili, Fadime Aydın Köse, Luciano Saso, Mohamed Akssira, Franck Suzenet, Mumin Alper Erdogan
Jazyk: angličtina
Rok vydání: 2018
Předmět:
0301 basic medicine
MAPK/ERK pathway
tumor cells
hydrogen peroxide
molecular structure
medicine.disease_cause
01 natural sciences
imidazo[2
cell survival
dose-response relationship
CH arylation
03 medical and health sciences
Western blot
Drug Discovery
akt signaling
triazines
medicine
oxidative stress
drug discovery3003 pharmaceutical science
MTT assay
Viability assay
humans
cultured
Protein kinase B
medicine.diagnostic_test
010405 organic chemistry
Chemistry
structure-activity relationship
apoptosis
1-c][1
drug
General Medicine
Molecular biology
0104 chemical sciences
organic chemistry
030104 developmental biology
Apoptosis
regioselective
Toxicity
cyclocondensation
imidazoles
4]triazines
imidazo[2
1-c][1
2
4]triazines

dose-response relationship
drug

stereoisomerism
tumor cells
cultured

pharmacology
Oxidative stress
Popis: 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 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 H2O2-induced toxicity by increasing Bcl-2/Bax ratio, regulating PI3-K/Akt cascade and inhibiting the ERK pathway.
Databáze: OpenAIRE