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Potent and selective inhibitors of the proteasome: dipeptidyl boronic acids.

Bioorganic & medicinal chemistry letters (1999-01-01)
J Adams, M Behnke, S Chen, A A Cruickshank, L R Dick, L Grenier, J M Klunder, Y T Ma, L Plamondon, R L Stein
RÉSUMÉ

Potent and selective dipeptidyl boronic acid proteasome inhibitors are described. As compared to peptidyl aldehyde compounds, boronic acids in this series display dramatically enhanced potency. Compounds such as 15 are promising new therapeutics for treatment of cancer and inflammatory diseases.

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Bortezomib