α,α-Difluoro-β-ketophosphonates as potent inhibitors of protein tyrosine phosphatase 1B
2004
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.
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