CK2α and CK2α′ subunits differ in their sensitivity to 4,5,6,7-tetrabromo- and 4,5,6,7-tetraiodo-1H-benzimidazole derivatives

The goal of this study was to test the inhibitory activity of a series of tetrahalogenobenzimidazoles, including a number of novel derivatives, on individual catalytic subunits of human CK2. 4,5,6,7-tetrabromo- and 4,5,6,7-tetraiodo-1H-benzimidazoles and their newly obtained N1- and 2-S-carboxyalkyl derivatives showed potent inhibitory activity against both these subunits. CK2α′ was up to 6 times more sensitive to the studied compounds than CK2α. The investigated iododerivatives showed, in most cases, stronger inhibitory properties than the respective brominated congeners, but the differences showed considerable dependence on the protein substrate used.

4,5,6,7-tetrabromo- and 4,5,6,7-tetraiodo-1H-benzimidazoles and their newly obtained N1- and 2-S-carboxyalkyl derivatives showed potent inhibitory activity against human protein kinase CK2 catalytic subunits. Among newly synthesized compounds 5c and 5e exert the highest anti-CK2 activity. CK2α′ was up to 6 times more sensitive to the studied compounds than CK2α.Figure optionsDownload as PowerPoint slideHighlights
► Novel benzimidazole derivatives were synthesized and biologic activity evaluated.
► In most cases CK2α′ subunit was more sensitive to the inhibitors.
► Differences were observed dependent from the examined substrate.