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

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

Volume: 12 Issue: 10

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

Affiliation:

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

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.

Cite this article as:

Zhao Dong-Hai, Zhang JIan, Zhang Lei, Li Da-Peng, Peng Zhou and Guan Li-Ping, Synthesis and Biological Evaluation of 2´-Hydroxy-4´,6´-Diprenyloxychal-Cone Derivatives as Potent CDC25B and PTP1B Inhibitors, Letters in Drug Design & Discovery 2015; 12 (10) . https://dx.doi.org/10.2174/1570180812666150723002629