Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 12, Pages 3220-3224Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.04.103
Keywords
Proteasome; Boron peptides; Chymotrypsin-like activity
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Funding
- Ministry of Education, Science, Sports, Culture and Technology [18350090]
- Grants-in-Aid for Scientific Research [18350090] Funding Source: KAKEN
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A series of boron peptides 11, 13, 15 and 17 were designed and synthesized as proteasome inhibitors based on the structure of Belactosin C. Matteson homologation was a key step in the synthesis of the boron peptides. Compounds 11a and 13 showed significant inhibition of 20S proteasome chymotrypsin-like (beta 5) activity (IC(50) = 0.28 and 0.51 mu M, respectively). Furthermore, like PS-341, compound 11a increased the G2/M cell distribution. A biparametric cytofluorimetric analysis with FITC-labeled annexin V and propidium iodide showed induction of apoptosis by compound 11a at >1 mu M concentrations of compound. (C) 2009 Elsevier Ltd. All rights reserved.
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