Synthesis of selenophene derivatives as novel CHK1 inhibitors

A series of selenophene derivatives 3 were synthesized as potential CHK1 inhibitors. The effects of substitution on the 4′- or 5′-position of selenophene moiety and shifting the hydroxyl group position on C6- phenolic ring of oxindole were explored. This study led to the discovery of the most potent CHK1 inhibitors 29–33 and 39–43, which had IC50 values in the subnanomolar range.

A series of selenophene derivatives (i.e., 31) are reported as potent inhibitors of CHK1 kinase.Figure optionsDownload as PowerPoint slide