title: Alpha,alpha-difluoro-beta-ketophosphonates as potent inhibitors of protein tyrosine phosphatase 1B.
abstract: 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.
authors.affiliation: Affymax, Inc., 4001 Miranda Avenue, Palo Alto, CA 94304, USA. xli@galieopharma.com
authors.forename: Xianfeng
authors.initials: X
authors.lastname: Li
authors.forename: Ashok
authors.initials: A
authors.lastname: Bhandari
authors.forename: Christopher P
authors.initials: CP
authors.lastname: Holmes
authors.forename: Anna K
authors.initials: AK
authors.lastname: Szardenings
mesh_terms: D002384:Catalysis; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D063065:Organophosphonates / Q000737:chemistry / Q000494:pharmacology*; D017027:Protein Tyrosine Phosphatases / Q000037:antagonists & inhibitors*
chemical_list: D004791:Enzyme Inhibitors; D063065:Organophosphonates; D017027:Protein Tyrosine Phosphatases