新型 1,2,4-三唑啉-3-酮衍生物的合成、表征及体外抗癌活性评价。
Synthesis, characterization and in vitro anticancer evaluation of novel 1,2,4-triazolin-3-one derivatives.
机构信息
Department of Studies in Chemistry, Karnatak University, Pavate Nagar, Dharwad-580003, India.
出版信息
Eur J Med Chem. 2013 Apr;62:232-40. doi: 10.1016/j.ejmech.2013.01.004. Epub 2013 Jan 11.
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).
一系列新型 2-(4-氯苯基)-5-甲基-4-(2-胺/氧基-乙基)-2,4-二氢-[1,2,4]三唑-3-酮（5a-t）被合成，并在单一高剂量（10(-5) M）浓度下对 NCI-60 人肿瘤细胞系进行了初步细胞毒性测定，研究了所得化合物的体外抗癌作用。在所测试的化合物（5a-e、5g-h、5k、5p）中，化合物 5g（NSC：761736/1）在五个不同的最小浓度下进一步根据五个剂量标准进行了评估，针对 60 个人类肿瘤细胞系的全谱，该化合物对白血病（GI50：1.10 μM）、非小细胞肺癌（GI50：1.00 μM）、肾细胞癌（GI50：1.00 μM）、结肠癌（GI50：1.66 μM）、中枢神经系统癌症（GI50：1.36 μM）、黑色素瘤（GI50：1.82 μM）、卵巢癌（GI50：1.64 μM）和乳腺癌（GI50：1.69 μM）均具有活性。
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