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3-(6-Phenylimidazo [2,1-b][1,3,4]thiadiazol-2-yl)-1HIndole derivatives as new anticancer agents in the treatment of pancreatic ductal adenocarcinoma

  • Authors: Cascioferro S.; Li Petri G. ; Parrino B.; El Hassouni B.; Carbone D.; Arizza V.; Perricone U.; Padova A.; Funel N.; Peters G.J.; Cirrincione G.; Giovannetti E.; Diana P.
  • Publication year: 2020
  • Type: Articolo in rivista
  • Key words: Antiproliferative activity; Imidazo[2,1-b][1,3,4]thiadiazole derivatives; Indole compounds; Migration assay; Pancreatic cancer; Resistance
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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 ╬╝M, 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.