title: Synthesis of salinosporamide A and its analogs as 20S proteasome inhibitors and SAR summarization.
abstract: Salinosporamide A (4), a secondary metabolite of the marine actinomycete Salinispora tropica, is a potent inhibitor of 20S proteasome that is currently in clinical trials for the treatment of cancers. Herein, we described various synthetic strategies of 4 and summarized the SAR of 4 and its analogs.
authors.affiliation: State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing, China.
authors.forename: Yuheng
authors.initials: Y
authors.lastname: Ma
authors.forename: Lili
authors.initials: L
authors.lastname: Qu
authors.forename: Zhenming
authors.initials: Z
authors.lastname: Liu
authors.forename: Liangren
authors.initials: L
authors.lastname: Zhang
authors.forename: Zhenjun
authors.initials: Z
authors.lastname: Yang
authors.forename: Lihe
authors.initials: L
authors.lastname: Zhang
mesh_terms: D007783:Lactones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011480:Protease Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D061988:Proteasome Inhibitors; D011758:Pyrroles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D007783:Lactones; D011480:Protease Inhibitors; D061988:Proteasome Inhibitors; D011758:Pyrroles; C475865:marizomib