ИСТИНА

Preparation of cis-imidazoline derivatives using the reaction of aromatic aldehydes with ammonia is a convenient and simple synthesis of the imidazolines, precursors of the known inhibitors Mdm2-p53 interaction. We report docking studies, synthetic approach, cytotoxicity and mechanism of action analysis. Docking studies showed the possibility of proposed structures to occupy p53 binding pockets. Using the proposed synthetic approach, we synthesized various cis-imidazoline structures containing halogens, alkoxy and hydroxy groups and investigated their cytotoxicity. Despite the fact that both derivatives (R = 4-Cl, 4-MeO) showed cytotoxicity and increased p53 level, chlorine derivatives induced necrotic cell death, while alkoxy derivative was not toxic and demonstrated the best efficacy for p53 stabilization.