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Sulfonylated aminothiazoles as new small molecule inhibitors of protein phosphatases
P Wipf1, D C Aslan, E C Southwick
1Department of Chemistry, University of Pittsburgh, PA 15260, USA. pwipf@pitt.edu
Bioorganic & Medicinal Chemistry Letters
|February 24, 2001
Abstract:
Based on a previously identified lead structure, SC-alphaalphadelta9, we have developed a versatile new chemical scaffold that can be readily modified to generate libraries of both Tyr and dual specificity phosphatase inhibitors with reduced molecular weight and lipophilicity. The most potent analogue identified to date, aminothiazole 8z, inhibits the dual specificity phosphatase Cdc25B with a Ki of 4.6+/-0.4 microM and a Hill coefficient of 2.