Biological Evaluation of the Antiproliferative and Anti-migratory Activity of a Series of 3-(6-Phenylimidazo[2,1-][1,3,4]thiadiazol-2-yl)-1-indole Derivatives Against Pancreatic Cancer Cells.

Heterocyclic rings are recognized as key components of many natural, semi-synthetic and synthetic molecules with a broad spectrum of biological activities. Among these molecules, the indole and imidazo[2,1-b][1,3,4]thiadiazole systems have recently been described as useful scaffolds for the design of anticancer agents. Herein the antitumor activity of a series of 3-(6-phenylimidazo[2,1-b][1,3,4]thiadiazol-2-yl)-1H-indoles, designed as hybrid structures, was assessed. Seven out of 10 compounds () were submitted to National Cancer Institute (NCI). Remarkably, compound showed antiproliferative activity against the full panel of sixty human cancer lines, with half-maximal inhibitory concentration of between 1.67 and 10.3 μM. Further studies showed antiproliferative activity of and of three additional compounds , and , with different substituents on the indole nucleus and phenyl ring, against three pancreatic cancer cell lines. In particular, derivatives and inhibited both proliferation and migration of SUIT-2 cells at concentrations lower than 10 μM. In conclusion, new indole derivatives are characterized by in vitro antitumor activity, supporting future mechanistic studies.