Discovery Of A Potent And Highly Specific Beta(2) Proteasome Inhibitor From A Library Of Copper Complexes

We reported the synthesis, characterization and biological activity of several copper(II) Schiff base complexes, which exhibit high proteasome inhibitory activities with particular selectivity of beta(2) subunit. Structure-activity relationships information obtained from complex Na-2[Cu(a4s1)] demonstrated that distinct bonding modes in beta(2) and beta(5) subunits determines its selectivity and potent inhibition for beta(2) subunit. (C) 2016 Elsevier Ltd. All rights reserved.