【摘要】 本文设计并合成了一系列吡咯啉酮类似物,这些化合物可能作为Michael受体与蛋白酶体活性位点Thr1O~γ不可逆结合,从而抑制蛋白酶体的活性。虽然活性测试结果显示这些化合物对蛋白酶体的抑制活性很弱,但是可以通过吡咯啉酮类化合物进一步的结构优化来提高对蛋白酶体的抑制活性。更多还原

【Abstract】 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 that the compounds display poor inhibitory activity towards the proteasome active sites,pyrrolidinone analogs might still be modified to be potential 20S proteasome inhibitors.更多还原