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Synthesis and anticancer evaluation of some new hydrazone derivatives of 2,6-dimethylimidazo[2,1-b][1,3,4]thiadiazole-5-carbohydrazide.
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2003 Jul-Aug
Terzioglu, Nalan, Gursoy, Aysel

In this study, some novel 2,6-dimethyl-N'-substituted phenylmethylene-imidazo[2,1-b][1,3,4]thiadiazole-5-carbohydrazides (3a-3h) were synthesized from 2,6-dimethylimidazo-[2,1-b][1,3,4]thiadiazole-5-carbohydrazide (2). The newly synthesized compounds (3a-3h) were evaluated in the National Cancer Institute's 3-cell line, one dose in vitro primary cytotoxicity assay. Compounds 3c and 3h which passed the criteria for activity in this assay (20-29% growth percentages) were scheduled automatically for evaluation against the full panel of 60 human tumor cell lines at a minimum of five concentrations at 10-fold dilutions. Sulforhodamine B (SRB) protein assay was used to estimate cell stability or growth. 2,6-Dimethyl-N'-(2-hydroxyphenylmethylidene)imidazo[2,1-b][1,3,4]thiadiazole-5-ca rbohydrazide (3c) showed the most favorable cytotoxicity. This compound demonstrated the most marked effects in the National Cancer Institute's 60 human tumor cell line in vitro screen on an ovarian cancer cell line (OVCAR log(10)GI(50) value -5.51).

中文翻译:

2,6-二甲基咪唑并[2,1-b] [1,3,4]噻二唑-5-碳酰肼的一些new衍生物的合成及抗癌作用评估。

在这项研究中,由2,6-合成了一些新颖的2,6-二甲基-N'-取代的苯基亚甲基-咪唑并[2,1-b] [1,3,4]噻二唑-5-碳酰肼(3a-3h)。二甲基咪唑-[2,1-b] [1,3,4]噻二唑-5-碳酰肼(2)。新合成的化合物(3a-3h)在美国国家癌症研究所(National Cancer Institute)的3细胞株中进行了一剂体外原代细胞毒性试验的评估。将通过该测定法中的活性标准(20-29%的生长百分比)的化合物3c和3h自动排定,以针对60种人类肿瘤细胞系的全系列进行评估,以至少5种浓度,10倍稀释度进行。Sulforhodamine B(SRB)蛋白测定用于评估细胞稳定性或生长。2,6-二甲基-N'-(2-羟基苯基亚甲基)咪唑并[2,1-b] [1,3,4]噻二唑-5-钙硼酰肼(3c)显示出最有利的细胞毒性。
更新日期:2017-01-31
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