MARIUS MIOC, SORIN AVRAM, VASILE BERCEAN, MIHAELA BALAN PORCARASU, CODRUTA SOICA, RAZVAN SUSAN,LUDOVIC KURUNCZI SYNTHESIS, CHARACTERIZATION AND ANTIPROLIFERATIVE ACTIVITY ASSESSMENT OF A NOVEL 1H-5-MERCAPTO-1,2,4 TRIAZOLE DERIVATIVE Angiogenesis plays an important function in tumor proliferation, one of the main angiogenic promoters being the vascular endothelial growth factor (VEGF) which activates specific receptors, particularly VEGFR-2. Thus, VEGFR-2 has become an essential therapeutic target in the development of new antitumor drugs. 1,2,4-triazoles show a wide range of biological activities, including antitumor effect, which was documented by numerous reports. In the current study the selection of 5-mercapto-1,2,4-triazole structure (1H-3-styryl-5-benzylidenehydrazino-carbonyl-methylsulfanil-1,2,4-triazole, Tz3a.7) was conducted based on molecular docking that emphasized it as suitable ligand for VEGFR-2 and EGFR1 receptors. Compound Tz3a.7 was synthesized and physicochemically and biologically evaluated thus revealing a moderate antiproliferative activity against breast cancer cell line MDA-MB-231.
Keywords: 1,2,4-triazole, antiproliferative, angiogenesis, breast cancer, VEGFR-2, EGFR1