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)
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 biol...
National Basic Research Program of China(Grant No.2012CB518000);the National Natural Science Foundation of China(Grant No.21172012);the Specialized Research Fund for the Doctoral Program of Higher Education of China(Grant No.20120001110010)
As important constitutes in many drugs, piperazine comprised compounds are of great interest for drug design. In this paper, two piperazine-based compounds were synthesized for the first time, with different strategie...
National Natural Science Foundation of China(Grant No. 21002002);Specialized Research Fund for the Doctoral Program of Higher Education of China (Grant No. 200800011057)
Computer aided fragment-based lead discovery has been successfully applied to the design of inhibitors of aspartyl protease enzyme β-secretase(BACE1).A benzimidamide fragment,which binds to the two catalytic aspart...
A novel series of pyrrolidinone analogs that are designed as Michael addition acceptors to react irreversibly with the proteasome active site Thr1O~γhave been synthesized.Although biological evaluation results show t...
National Natural Science Foundation of China (Grant No.20772008 and 30772650)
A series of acyclic analogs of natural product Syringolin A (SylA) were designed and synthesized during our synthetic efforts for SylA. These acyclic analogs were prepared through a seven-step linear strategy, with ...
National Natural Science Foundation of China (Grant No.20772008 and 30772650)
Based upon the crystal structure of a previously reported fragment hit that binds to Corresponding author. β-secretase, a novel series of non-peptidic small-molecule β-secretase inhibitors, namely hexahydropyrimidin...