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

Author(s): Yuheng Ma , Lili Qu , Zhenming Liu , Liangren Zhang , Zhenjun Yang , Lihe Zhang .

Journal Name: Current Topics in Medicinal Chemistry

Volume 11 , Issue 23 , 2011

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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

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Article Details

Year: 2011
Page: [2906 - 2922]
Pages: 17
DOI: 10.2174/156802611798281302
Price: $58

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