Design, Synthesis and Biological Evaluation of Stilbene Derivatives as Novel Inhibitors of Protein Tyrosine Phosphatase 1B
作者： Haibing He , Yinghua Ge , Hong Dai , Song Cui , Fei Ye
DOI: 10.3390/MOLECULES21121722
关键词:
摘要: By imitating the scaffold of lithocholic acid (LCA), a natural steroidal compound displaying Protein Tyrosine Phosphatase 1B (PTP1B) inhibitory activity, series stilbene derivatives containing phenyl-substituted isoxazoles were designed and synthesized. The structures title compounds confirmed by 1H-NMR, 13C-NMR HRMS. Activities evaluated on PTP1B homologous enzyme TCPTP using colorimetric assay. Most target had good activities against PTP1B. Among them, 29 (IC50 = 0.91 ± 0.33 μM), characterized 5-(2,3-dichlorophenyl) isoxazole moiety, exhibited an activity about 14-fold higher than lead LCA 4.2-fold selectivity over TCPTP. Compound was identified as competitive inhibitor with Ki value 0.78 μM in kinetic studies.
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