α-Ketocarboxylic acid-based inhibitors of protein tyrosine phosphatases
YT Chen, MB Onaran, CJ Doss, CT Seto
Index: Chen, Yen Ting; Onaran; Doss, Christopher J.; Seto, Christopher T. Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 14 p. 1935 - 1938
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Citation Number: 30
Abstract
A series of aryl α-ketocarboxylic acids was synthesized and investigated as inhibitors for the protein tyrosine phosphatase from Yersinia enterocolitica. IC50 values for these compounds range from 79 to 2700μM. Larger aromatic groups, and aromatic groups with high electron density, lead to more potent inhibitors. In general, the related aryl α-hydroxycarboxylic acids show lower activity.
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