Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 26, Issue 23, Pages 5780-5784Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2016.10.043
Keywords
Proteasome inhibitors; Schiff base; Copper complex; Drug design; Structure-activity relationships
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Funding
- National Natural Science Foundation of China [21202003/21571007/21271013]
- Beijing Natural Science Foundation [7162110]
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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.
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