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 (GI50: 1.10 μM), Non-Small Cell Lung Cancer (GI50: 1.00 μM), Renal Cancer (GI50: 1.00 μM), Colon Cancer (GI50: 1.66 μM), CNS Cancer (GI50: 1.36 μM), Melanoma (GI50: 1.82 μM), Ovarian Cancer (GI50: 1.64 μM) and Breast Cancer (GI50: 1.69 μM).

A series of novel 1,2,4-triazolin-3-one appended to different heterocyclic/aryl moieties (5a–t) were synthesized and in vitro anticancerous action was studied against NCI-60 Human Tumor Cell Lines. The compound 5g comprising 1,2,4-triazolin-3-one appended to 4-methylcoumarin ring has shown potent anticancer activity against various cell lines. Figure optionsDownload as PowerPoint slideHighlights
► Novel 1,2,4-triazolin-3-one derivatized with various heterocycles/aryl groups were synthesized.
► In vitro anticancer activity against NCI-60 human tumor cell lines was done.
► The compound 5g comprising 4-methylcoumarin ring has shown potent anticancer activity.