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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Published on: 01 March, 2012
Page: [2906 - 2922]