A series of 2,5,6-substituted imidazo[2,1-b][1,3,4]thiadiazole derivatives have been prepared and were tested for antiproliferative activity on cancer cells at the National Cancer Institute. Results showed that molecules with a benzyl group at position 2, exhibited an increase in activity for the introduction of a formyl group at the 5 position. The compound 2-benzyl-5-formyl-6-(4-bromophenyl)imidazo[2,1-b][1,3,4]thiadiazole 22 has been chosen for understanding the mechanism of action by various molecular and cellular biology studies. Results obtained from cell cycle evaluation analysis, analysis of mitochondrial membrane potential and Annexin V-FITC by flow cytometric analysis, ROS production and expression of apoptotic and DNA-repair proteins suggested that compound 22 induced cytotoxicity by activating extrinsic pathway of apoptosis, however, without affecting cell cycle progression.

已经制备了一系列的2,5,6-取代的咪唑并[2,1- b ] [1,3,4]噻二唑衍生物，并在美国国家癌症研究所测试了其对癌细胞的抗增殖活性。结果表明，在2位具有苄基的分子表现出在5位引入甲酰基的活性增加。化合物2-苄基-5-甲酰基-6-（4-溴苯基）咪唑并[2,1- b ] [1,3,4]噻二唑22已通过各种分子和细胞生物学研究选择了理解作用机理的化合物。从细胞周期评估分析，通过流式细胞术分析线粒体膜电位和膜联蛋白V-FITC，ROS产生以及凋亡和DNA修复蛋白表达获得的结果表明，化合物22通过激活细胞凋亡的外在途径诱导细胞毒性。影响细胞周期进程。