Discovery of Carboranes as Inducers of 20S Proteasome Activity



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The carborane framework gives analogues able to induce 20S proteasome activities. A series of ortho-carboranylphenoxy derivatives were synthesized as 20S proteasome agonists, and carborane derivatives 11 a and 11 b were found to be potent inducers of the β1 and β2 activities of the 20S proteasome. Since small-molecule proteasome activators have not been developed, the carboranes described here have potential as chemical probes for the investigation of proteasome-dependent degradation pathways.