Generic placeholder image

Current Topics in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

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 and Lihe Zhang

Volume 11, Issue 23, 2011

Page: [2906 - 2922] Pages: 17

DOI: 10.2174/156802611798281302

Price: $65

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


Rights & Permissions Print Cite
© 2024 Bentham Science Publishers | Privacy Policy