Synthesis, characterization and in vitro anticancer evaluation of novel 1,2,4-triazolin-3-one derivatives
Synthesis, characterization and in vitro anticancer evaluation of novel 1,2,4-triazolin-3-one derivatives
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DOI：
10.1016/j.ejmech.2013.01.004
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发表时间：
2013-04-01
影响因子：
6.7
通讯作者：
Hunnur, Raveendra K.
中科院分区：
文献类型：
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作者：
Kattimani, Pramod P.;Kamble, Ravindra R.;Hunnur, Raveendra K.
本文合成了一系列新的2-（4-氯苯基）-5-甲基-4-（2-胺/氧乙基）-2，4-二氢-[1，2，4]三唑-3-酮（5a-t），并研究了它们在高剂量（10（-5）M）下对NCI-60人肿瘤细胞株的体外抗肿瘤作用。在测试的化合物中，（5a-e，5g-h，5 k，5 p），化合物5g（NSC：761736/1）在5种不同的最小浓度下针对全部60种人肿瘤细胞系的5种剂量标准进行了进一步评价，所述细胞系显示出抗白血病（GI（50）：1.10 μ M）、非小细胞肺癌（GI（50）：00 μ M）、肾癌（GI（50）：1.00 μ M）、结肠癌（GI（50）：1.66 μ M）、CNS癌（GI（50）：1.36 μ M）、黑素瘤（GI（50）：1.82 μ M）、卵巢癌（GI（50）：1.64 μ M）和乳腺癌（GI（50）：1.69 μ M）。(C)2013年Elsevier Masson SAS。All rights reserved.
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.