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 20 S proteasome inhibitors.
【基金】
The National Natural Science Foundation of China(Grant No.21202003);
the National Basic Research Program of China(Grant No.2012CB518000);
the Specialized Research Fund for the Doctoral Program of Higher Education of China(Grant No.20120001110010)
【更新日期】
2014-11-06
【分类号】
R914
【正文快照】
1.IntroductionProtein degradation plays a significant role inmaintaining biological homeostasis and regulation ofdifferent intracellular physiological processes.Besides,the ubiquitin-proteasome pathway(UPP)is proved asthe major proteolytic system in the c
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