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Synthesis of Salinosporamide A and Its Analogs as 20S Proteasome Inhibitors and SAR Summarization

[ Vol. 11 , Issue. 23 ]


Yuheng Ma, Lili Qu, Zhenming Liu, Liangren Zhang, Zhenjun Yang and Lihe Zhang   Pages 2906 - 2922 ( 17 )


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.


20S Proteasome, inhibitors, salinosporamide A, total synthesis, structure-activity relationship, biological homeostasis, cytosolic protein degradation, transmembrane proteins, eukaryotic proteasome, hydrophobic interactions, trimethylsilyl chloride, Corey's cyclohexenylzinc reagent, nucleophilic ring, mild benzylating agent, nucleophilic promoter


1State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.

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