Research progress of synthetic lactacystin and its analogs as β-lactone proteasome inhibitors  

β-内酯类蛋白酶体抑制剂乳胞素及其衍生物的合成研究进展（英文）

作　　者：王玉平[1] 朱晓伟[1] 辛健[1] 郭妍妍[1] 徐向楠[1] 马宇衡[1] 

机构地区：[1]内蒙古医科大学药学院药物化学教研室,内蒙古呼和浩特010110

出　　处：《Journal of Chinese Pharmaceutical Sciences》2017年第7期467-478,共12页中国药学（英文版）

基　　金：National Natural Science Foundation of China(Grant No.21362021);Inner Mongolia Natural Science Foundation(Grant No.2015MS0206)

摘　　要：As Bortezomib and Carfilzomib are approved to treat refractory multiple myeloma, 20 S proteasome has become a highly interested tumor therapeutic target. Because of drug resistance of Bortezomib and Carfilzomib, β-lactone natural products are used to treat cancer, arthritis, asthma, and Alzheimer’s diseases. Now the second generation drug candidates are developed, eg. Salinosporamide A（1）. This review is aiming to encapsulate the synthetic methods of β-lactone proteasome inhibitors, lactacystin（3） and its analogs.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。

关 键 词：LACTACYSTIN β-Lactone PROTEASOME INHIBITORS 

分 类 号：R914[医药卫生—药物化学]