acetamidines have been designed as CK1 inhibitors. Binding modes in the ATP pocket of CK1 were determined by molecular modeling. The synthetic approach involves sequential acylation of 2-aminobenzimidazoles followed by reaction of amides with Lawesson's reagent and iminosulfonylation of thioamides with sulfonyl azides. The iminosulfonylation was carried out in boiling ethanol with an equivalent ratio of azides and thioamides. The synthesized compounds were tested for their ability to inhibit CK1 isoforms in vitro and to inhibit the growth of tumor cell lines. Among the synthesized compounds, two products showed inhibitory abilities towards CK1δ and CK1ε.

No abstract