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Molecules 2016, 21(12), 1722; doi:10.3390/molecules21121722

Design, Synthesis and Biological Evaluation of Stilbene Derivatives as Novel Inhibitors of Protein Tyrosine Phosphatase 1B

College of Chemistry and Chemical Engineering, Nantong University, Nantong 226019, China
College of Life Sciences, Zhejiang Sci-Tech University, Hangzhou 310018, China
Authors to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 26 October 2016 / Revised: 7 December 2016 / Accepted: 12 December 2016 / Published: 16 December 2016
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [1902 KB, uploaded 16 December 2016]   |  


By imitating the scaffold of lithocholic acid (LCA), a natural steroidal compound displaying Protein Tyrosine Phosphatase 1B (PTP1B) inhibitory activity, a series of stilbene derivatives containing phenyl-substituted isoxazoles were designed and synthesized. The structures of the title compounds were confirmed by 1H-NMR, 13C-NMR and HRMS. Activities of the title compounds were evaluated on PTP1B and the homologous enzyme TCPTP by using a colorimetric assay. Most of the target compounds had good activities against PTP1B. Among them, compound 29 (IC50 = 0.91 ± 0.33 μM), characterized by a 5-(2,3-dichlorophenyl) isoxazole moiety, exhibited an activity about 14-fold higher than the lead compound LCA and a 4.2-fold selectivity over TCPTP. Compound 29 was identified as a competitive inhibitor of PTP1B with a Ki value of 0.78 μM in enzyme kinetic studies. View Full-Text
Keywords: protein tyrosine phosphatase 1B (PTP1B); lithocholic acid; stilbene; inhibitor protein tyrosine phosphatase 1B (PTP1B); lithocholic acid; stilbene; inhibitor

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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He, H.; Ge, Y.; Dai, H.; Cui, S.; Ye, F.; Jin, J.; Shi, Y. Design, Synthesis and Biological Evaluation of Stilbene Derivatives as Novel Inhibitors of Protein Tyrosine Phosphatase 1B. Molecules 2016, 21, 1722.

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