Synthesis and Biological Evaluation of Heterocyclic Ring-substituted Chalcone Derivatives as Novel Inhibitors of Protein Tyrosine Phosphatase 1B

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Protein tyrosine phosphatase 1B (PTP1B) is a key factor in negative regulation of the insulin pathway, and is a promising target for the treatment of type-II diabetes, obesity and cancer. Herein, compound () was first observed to have moderate inhibitory activity against PTP1B with an value of . To obtain more potent PTP1B inhibitors, we synthesized a series of chalcone derivatives using compound () as the lead compound. Compound () was 4.4-fold more potent than the lead compound (), and more potent than the positive control, ursolic acid (). These results may help to provide suitable drug-like lead compounds for the design of inhibitors of PTP1B as well as other PTPs.