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).
Department of Studies in Chemistry, Karnatak University, Pavate Nagar, Dharwad-580003, India.
Pramod P
PP
Kattimani
Ravindra R
RR
Kamble
Mahadevappa Y
MY
Kariduraganavar
Atukuri
A
Dorababu
Raveendra K
RK
Hunnur
D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D003374:Coumarins / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
C583779:2-(4-chlorophenyl)-5-methyl-4-(2-(4-methyl-2-oxo-2H-chromen-7-yloxy)ethyl)-2H-1,2,4-triazol-3(4H)-one; D000970:Antineoplastic Agents; D003374:Coumarins; D014230:Triazoles