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1: Bioorg Med Chem Lett. 2004 Aug 16;14(16):4301-6.Click here to read Links

Alpha,alpha-difluoro-beta-ketophosphonates as potent inhibitors of protein tyrosine phosphatase 1B.

Li X, Bhandari A, Holmes CP, Szardenings AK.

Affymax, Inc., 4001 Miranda Avenue, Palo Alto, CA 94304, USA. xli@galieopharma.com

A novel series of inhibitors that contain an aryl alpha,alpha-difluoro-beta-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 microM. These results demonstrate that aryl alpha,alpha-difluoro-beta-ketophosphonates are powerful phosphotyrosine mimetics for the development of potent PTP inhibitors.

PMID: 15261291 [PubMed - indexed for MEDLINE]