当硼替佐米和卡非佐米被FDA批准用于治疗多发性骨髓瘤后,20S蛋白酶体已经作为靶点引起了关注,但这两种药物存在耐药性。作为第二代候选药物,从天然产物中提取得到的β-内酯类蛋白酶抑制剂被用于癌症、关节炎、哮喘和阿尔茨海默病的治疗,代表药物为Salinosporamide A(1)。本文综述了具有β-内酯结构的乳胞素及其衍生物的合成方法。 When bortezomib and carfilizamide are approved by the FDA for the treatment of multiple myeloma, the 20S proteasome has attracted attention as a target, but both drugs are resistant. As a second-generation candidate, β-lactone protease inhibitors extracted from natural products are used in the treatment of cancer, arthritis, asthma and Alzheimer’s disease, representing the drug Salinosporamide A (1). This review summarizes the synthesis of lactacystin and its derivatives with β-lactone structure.