Sulfonylated aminothiazoles as new small molecule inhibitors of protein phosphatases

P Wipf, DC Aslan, EC Southwick, JS Lazo

Index: Wipf, Peter; Aslan, Diana C.; Southwick, Eileen C.; Lazo, John S. Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 3 p. 313 - 317

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Citation Number: 23

Abstract

Based on a previously identified lead structure, SC-ααδ9, 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 μM and a Hill coefficient of 2.