Sulfonylated aminothiazoles as new small molecule inhibitors of protein phosphatases

P Wipf, DC Aslan, EC Southwick, JS Lazo

文献索引：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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被引用次数: 23

摘要

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.