Synthesis and Cytotoxicity in Vitro of<i>N</i>-Aryl-4-(<i>tert</i>-butyl)-5-(1<i>H</i>-1,2,4-triazol-1-yl)thiazol-2-amine
作者:Jiao Ye、Meng-Wu Xiao、Xuan-Qing Xie、Shen-Yi Qiu、Ming-Chong Dai、Wan Li、Fang Shen、Ai-Xi Hu
DOI:10.1002/jccs.201400395
日期:2015.7
A series of novel N‐aryl‐4‐(tert‐butyl)‐5‐(1H‐1,2,4‐triazol‐1‐yl)thiazol‐2‐amines synthesized in a green way. H2O2‐NaBr Brominating circulatory system was used in the synthesis of the key intermediate in a mild condition. All of the target compounds were confirmed by 1H NMR and elemental analysis and tested for their cytotoxicity against two different human cancer cell lines. The cytotoxicity assay
以绿色方式合成的一系列新型N-芳基-4-(叔丁基)-5-(1 H -1,2,4-三唑-1-基)噻唑-2-胺。H 2 O 2 -NaBr溴化循环系统用于温和条件下关键中间体的合成。所有目标化合物均通过1 H NMR和元素分析确认,并测试了其对两种不同人类癌细胞系的细胞毒性。细胞毒性测定表明,某些标题化合物显示出中等至强的细胞毒性活性。化合物2i是最有效的化合物,针对Hela细胞的IC 50值为9μM,针对Hela细胞的IC 50值为15μMBel–7402细胞,分别。