4.7 Article

Proteasome inhibition in human breast cancer cells with high catechol-O-methyltransferase activity by green tea polyphenol EGCG analogs

Journal

BIOORGANIC & MEDICINAL CHEMISTRY
Volume 18, Issue 3, Pages 1252-1258

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2009.12.034

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Funding

  1. Natural Sciences and Engineering Research Council of Canada (NSERC)
  2. National Cancer Institute [1R01CA120009, 3R01CA120009-04S1]

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A pro-drug 8 of a synthetic analog 7 is more active in its antiproliferative activity against human breast cancer MDA-MB-231 cells possessing high catechol-O-methyltransferase (COMT) activity than the prodrugs of EGCG and the analog 5. The higher activity of 8 is attributed to it not being a substrate of COMT. (C) 2009 Elsevier Ltd. All rights reserved.

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