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3-(6-Phenylimidazo [2,1-b][1,3,4]thiadiazol-2-yl)-1H-Indole Derivatives as New Anticancer Agents in the Treatment of Pancreatic Ductal Adenocarcinoma
Molecules ( IF 4.2 ) Pub Date : 2020-01-14 , DOI: 10.3390/molecules25020329 Stella Cascioferro 1 , Giovanna Li Petri 1, 2 , Barbara Parrino 1 , Btissame El Hassouni 2 , Daniela Carbone 1 , Vincenzo Arizza 1 , Ugo Perricone 3 , Alessandro Padova 3 , Niccola Funel 4 , Godefridus J Peters 2 , Girolamo Cirrincione 1 , Elisa Giovannetti 2, 4 , Patrizia Diana 1
Molecules ( IF 4.2 ) Pub Date : 2020-01-14 , DOI: 10.3390/molecules25020329 Stella Cascioferro 1 , Giovanna Li Petri 1, 2 , Barbara Parrino 1 , Btissame El Hassouni 2 , Daniela Carbone 1 , Vincenzo Arizza 1 , Ugo Perricone 3 , Alessandro Padova 3 , Niccola Funel 4 , Godefridus J Peters 2 , Girolamo Cirrincione 1 , Elisa Giovannetti 2, 4 , Patrizia Diana 1
Affiliation
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：
3-(6-Phenylimidazo [2,1-b][1,3,4]thiadiazol-2-yl)-1H-Indole 衍生物作为治疗胰腺导管腺癌的新型抗癌药物
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 (PDAC) 细胞的体外抗增殖活性，包括 SUIT-2、Capan -1 和 Panc-1。化合物 9c 和 9l 在所有三种临床前模型中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，化合物 9c 在划痕伤口愈合试验中显着抑制了 SUIT-2 和 Capan-1 细胞的迁移率。总之，我们的结果将支持进一步研究以增加咪唑[2,1-b][1,3，
更新日期：2020-01-14
中文翻译：
3-(6-Phenylimidazo [2,1-b][1,3,4]thiadiazol-2-yl)-1H-Indole 衍生物作为治疗胰腺导管腺癌的新型抗癌药物
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 (PDAC) 细胞的体外抗增殖活性，包括 SUIT-2、Capan -1 和 Panc-1。化合物 9c 和 9l 在所有三种临床前模型中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，化合物 9c 在划痕伤口愈合试验中显着抑制了 SUIT-2 和 Capan-1 细胞的迁移率。总之，我们的结果将支持进一步研究以增加咪唑[2,1-b][1,3，
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