A new series of imidazo[2,1-b][1,3,4]thiadiazole derivatives was efficiently synthesized and screened for their in vitro antiproliferative activity on a panel of pancreatic ductal adenocarcinoma (PDAC) cells, including SUIT-2, Capan-1 and Panc-1. Compounds 9c and 9l, showed relevant in vitro antiproliferative activity on all three pre-clinical models with half maximal inhibitory concentration (IC50) ranging from 5.11 to 10.8 µM, while the compounds 9e and 9n were active in at least one cell line. In addition, compound 9c significantly inhibited the migration rate of SUIT-2 and Capan-1 cells in the scratch wound-healing assay. In conclusion, our results will support further studies to increase the library of imidazo [2,1-b][1,3,4] thiadiazole derivatives for deeper understanding of the relationship between biological activity of the compounds and their structures in the development of new antitumor compounds against pancreatic diseases.

中文翻译：

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3-(6-苯基咪唑[2,1-b][1,3,4]噻二唑-2-基)-1H-吲哚衍生物作为新型抗癌药物治疗胰腺导管腺癌


高效合成了一系列新的咪唑并[2,1-b][1,3,4]噻二唑衍生物，并筛选了它们对一组胰腺导管腺癌细胞（PDAC）（包括 SUIT-2、Capan）的体外抗增殖活性-1 和 Panc-1。化合物 9c 和 9l 在所有三种临床前模型上均显示出相关的体外抗增殖活性，半数抑制浓度 (IC50) 范围为 5.11 至 10.8 µM，而化合物 9e 和 9n 在至少一种细胞系中具有活性。此外，在划痕伤口愈合试验中，化合物9c显着抑制SUIT-2和Capan-1细胞的迁移速率。总之，我们的结果将支持进一步的研究，以增加咪唑并[2,1-b][1,3,4]噻二唑衍生物的库，以更深入地了解化合物的生物活性与其结构之间的关系，以开发针对胰腺疾病的新抗肿瘤化合物。