New biological investigations on triazol-imidazo[1,2-b]pyrazole scaffold

The 1,2,4-triazole scaffold is a key pharmacophore widely present in a broad range of biologically active compounds, including anticancer agents. In previous studies, we demonstrated the potential of the 1,2,4-triazole nucleus when linked to an imidazo-pyrazole scaffold for the design of biologically active compounds. In particular, compounds 1 showed significant anticancer activity, especially against melanoma cell lines, thus confirming the medchem attractiveness of the triazol-imidazo[1,2-b]pyrazole core. To further extend the structure-activity relationships (SARs) of 1, we designed and synthesized novel analogues 2 in which the triazole nucleus was functionalized with a more embedded thioethyl substituent. The new compounds were evaluated for anticancer activity across different cancer cell lines and for the inhibitory effects on aggregation and ROS production on human platelets that represent a good biological model to assay potential anti-inflammatory and anticancer drugs.