Journal of Chinese Pharmaceutical Sciences ›› 2014, Vol. 23 ›› Issue (9): 626-630.DOI: 10.5246/jcps.2014.09.080

• Original articles • Previous Articles     Next Articles

Design, synthesis and biological evaluation of sulfonamide flavone derivatives as potential 20S proteasome inhibitors

Guanyu Yang, Qi Sun, Chao Wang, Lei Liang*, Fengrong Xu, Yan Niu, Ping Xu*   

  1. Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China
  • Received:2014-04-15 Revised:2014-05-26 Online:2014-09-23 Published:2014-05-30
  • Contact: Tel.: 86-10-82802632, Fax: 86-10-82801117
  • Supported by:
    The National Natural Science Foundation of China (Grant No. 21202003), the National Basic Research Program of China (Grant No. 2012CB518000) and the Specialized Research Fund for the Doctoral Program of Higher Education of China (Grant No. 20120001110010).


A new series of sulfonamide flavone derivatives are designed as non-covalent inhibitors of proteasome assisted with computer-aided drug design (CADD). The desired compounds were synthesized successfully and the biological evaluation was subsequently accomplished. The results showed negligible improvement from our lead compound (IC50 for β5 subunit was 14.0 μM). Thus, these flavone derivatives might be improved as potential 20S proteasome inhibitors.

Key words: Sulfonamide flavone derivatives, Non-covalent inhibitor, CADD, 20S proteasome inhibitor, Selectivity

CLC Number: