α-Ketocarboxylic acid-based inhibitors of protein tyrosine phosphatases

Bioorganic & Medicinal Chemistry Letters
2001.0

Abstract

A series of aryl alpha-ketocarboxylic acids was synthesized and investigated as inhibitors for the protein tyrosine phosphatase from Yersinia enterocolitica. IC(50) values for these compounds range from 79 to 2700 microM. Larger aromatic groups, and aromatic groups with high electron density, lead to more potent inhibitors. In general, the related aryl alpha-hydroxycarboxylic acids show lower activity.

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