Synthesis, characterization and in vitro anticancer evaluation of novel 1,2,4-triazolin-3-one derivatives

A series of novel 2-(4-chlorophenyl)-5-methyl-4-(2-amine/oxy-ethyl)-2,4-dihydro-[1,2,4]triazol-3-one (5a-t) were synthesized and in vitro anticancerous action of the resulting compounds was studied against NCI-60 Human Tumor Cell Line at a single high dose (10(-5) M) concentration for primary cytotoxicity assay. Among the tested compounds (5a-e, 5g-h, 5k, 5p), the compound 5g (NSC: 761736/1) was further evaluated for five dose criteria at five different minimal concentrations against the full panel of 60 human tumor cell lines which exhibited activity against Leukemia (GI(50): 1.10 mu M), Non-Small Cell Lung Cancer (GI(50): 1.00 mu M), Renal Cancer (GI(50): 1.00 mu M), Colon Cancer (GI(50): 1.66 mu M), CNS Cancer (GI(50): 1.36 mu M), Melanoma (GI(50): 1.82 mu M), Ovarian Cancer (GI(50): 1.64 mu M) and Breast Cancer (GI(50): 1.69 mu M). (C) 2013 Elsevier Masson SAS. All rights reserved.