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

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.

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