α,α‐Difluoro‐β‐ketophosphonates as Potent Inhibitors of Protein Tyrosine Phosphatase 1B.

Abstract A novel series of inhibitors that contain an aryl α,α-difluoro-β-ketophosphonate group has been synthesized and evaluated against protein tyrosine phosphatase 1B. These compounds exhibit strong inhibitory activity, the best of which has a K i value of 0.17 μM. These results demonstrate that aryl α,α-difluoro-β-ketophosphonates are powerful phosphotyrosine mimetics for the development of potent PTP inhibitors.