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。 In this paper, a series of pyrrolindone analogs were designed and synthesized. These compounds may act as irreversible binding of Michael receptor to Thr1O ~ γ, the active site of proteasome, thus inhibiting the activity of proteasome. Although the activity test results show that these compounds have weak inhibitory activity on the proteasome, the inhibitory activity on the proteasome can be enhanced by further structural optimization of the pyrrolinones.