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Synthesis and primary cytotoxicity evaluation of new imidazo[2,1-b]thiazole derivatives.
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2007 Mar , DOI: 10.1016/j.ejmech.2006.10.012
Elif Gürsoy , Nuray Ulusoy Güzeldemirci

A series of arylidenehydrazides (3a-3i) were synthesized from [6-(4-bromophenyl)imidazo[2,1-b]thiazol-3-yl]acetic acid hydrazide. The structures of new compounds were determined by analytical and spectral (IR, (1)H NMR, (13)C NMR, EIMS) methods. The synthesized compounds (3a-3i) were evaluated in the National Cancer Institute's 3-cell line, one dose in vitro primary cytotoxicity assay. Compounds 3a-3c, 3h and 3i which passed the criteria for activity in this assay were scheduled automatically for evaluation against the full panel of 60 human tumour cell lines at a minimum of five concentrations at 10-fold dilutions. Compounds 3c demonstrated the most marked effects on a prostate cancer cell line (PC-3, log(10)GI(50) value<-8.00).

中文翻译:

新型咪唑并[2,1-b]噻唑衍生物的合成及初步细胞毒性评估。

由[6-(4-溴苯基)咪唑并[2,1-b]噻唑-3-基]乙酸酰肼合成了一系列芳基酰肼(3a-3i)。通过分析和光谱(IR,(1)H NMR,(13)C NMR,EIMS)方法确定新化合物的结构。合成的化合物(3a-3i)在美国国家癌症研究所的3细胞株中进行了一次剂量的体外原代细胞毒性试验。将通过该测定法中的活性标准的化合物3a-3c,3h和3i自动排定,以针对全组的60种人类肿瘤细胞系进行评估,其浓度至少为5倍,稀释度为10倍。化合物3c对前列腺癌细胞系表现出最显着的作用(PC-3,log(10)GI(50)值<-8.00)。
更新日期:2017-01-31
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