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Protein tyrosine phosphatases (PTPs) together with protein tyrosine kinases (PTKs) regulate protein tyrosine phosphorylation. Their abnormal functions are involved in the initiation and maintenance of the oncogenic state in human. Several synthetic tetronic acid derivatives related to the natural product RK-682 (R)-1 (Figure 1) have been evaluated as inhibitors of dual-specificity phosphatases VHR and CDC-25B and four derivatives were shown to be the most potent inhibitors of CDC-25B described so far.

Synthesis of Six-membered Ring Analogues of RK-682 and Meldrum’s acid derivatives. Evaluation on the Inhibition of Protein Tyrosine Phosphatases