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
Current Topics in Medicinal Chemistry
Title: Synthesis of Salinosporamide A and Its Analogs as 20S Proteasome Inhibitors and SAR Summarization
Volume: 11 Issue: 23
Author(s): Yuheng Ma, Lili Qu, Zhenming Liu, Liangren Zhang, Zhenjun Yang and Lihe Zhang
Affiliation:
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
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.
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Cite this article as:
Ma Yuheng, Qu Lili, Liu Zhenming, Zhang Liangren, Yang Zhenjun and Zhang Lihe, Synthesis of Salinosporamide A and Its Analogs as 20S Proteasome Inhibitors and SAR Summarization, Current Topics in Medicinal Chemistry 2011; 11 (23) . https://dx.doi.org/10.2174/156802611798281302
DOI https://dx.doi.org/10.2174/156802611798281302 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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