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

[ Vol. 11 , Issue. 23 ]

Author(s):

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

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.

Keywords:

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

Affiliation:

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



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