Synthesis and Biological Evaluation of 2´-Hydroxy-4´,6´-Diprenyloxychal-Cone Derivatives as Potent CDC25B and PTP1B Inhibitors

Author(s): Dong-Hai Zhao, JIan Zhang, Lei Zhang, Da-Peng Li, Zhou Peng, Li-Ping Guan

Journal Name: Letters in Drug Design & Discovery

Volume 12 , Issue 10 , 2015

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Graphical Abstract:


A series of 2´-hydroxy-4´,6´-diisoprenyloxychalcone derivatives were synthesized and evaluated for inhibitory activities against CDC25B and PTP1B. The results displayed the most of them showed inhibitory activities against CDC25B (IC50=1.19–14.20 µg/mL) and PTP1B (IC50= 1.26–8.44µg /mL), respectively. Moreover, compound 2h displayed the most CDC25B and PTP1B inhibitory activity in vitro with IC50 values of 1.19 and 1.26 µg/mL, respectively, compared with reference drugs Na3VO4(IC50=1.09 µg/mL) and oleanolic acid (IC50=1.01 µg/mL). The results of selectivity experiments showed that the target compounds were selective inhibitors against CDC25B and PTP1B. Enzyme kinetic experiments demonstrated that compound 2h was a specific inhibitor with the typical characteristics of a mixed inhibitor.

Keywords: 2´-Hydroxy-4´, 6´-diprenyloxychalcone, synthesis, CDC25B, PTP1B, phosphatase inhibitors, enzyme kinetic.

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Article Details

Year: 2015
Published on: 12 October, 2015
Page: [864 - 871]
Pages: 8
DOI: 10.2174/1570180812666150723002629
Price: $65

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