Design, synthesis, and evaluation of bromo-retrochalcone derivatives as protein tyrosine phosphatase 1B inhibitors

A series of bromo-retrochalcones was designed, synthesized and evaluated as PTP1B inhibitors based on licochalcone A and E. Compounds 6, 12, 13, 14, 25, 36, 37, 39, and 41 showed potent inhibitory effects against PTP1B, and compound 37, the most potent among the series, had an IC50 value of 1.9 μM, about two-fold better than that of the positive control, ursolic acid.

Bromo-retrochalcone, 37 exhibited significant PTP1B inhibitory activity.Figure optionsDownload as PowerPoint slide