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Substitution of a triazole for the central olefin in biologically active stilbenes

  1. Author:
    Stockdale, David P
    Beutler,John
    Wiemer, David F

  2. Author Address

    Department of Chemistry University of Iowa, Iowa City, Iowa 52242-1294., Molecular Targets Program, Center for Cancer Research, NCI-Frederick, Frederick, MD 21702., Department of Chemistry University of Iowa, Iowa City, Iowa 52242-1294. Electronic address: david-wiemer@uiowa.edu.,
    1. Year: 2022
    2. Date: Sep 09
    3. Epub Date: 2022 09 09
  2. Journal: Bioorganic & Medicinal Chemistry Letters
    1. Pages: 128980
  4. Type of Article: Article
  5. Article Number: 128980
  1. Abstract:

    The stilbene moiety is commonly found in natural products and these compounds display an extraordinary range of biological activity. Efforts to derive useful drugs from stilbenes must address the potential liabilities of this structure, including a propensity for cis/trans isomerization. To identify olefin replacements that address this limitation while preserving biological activity we have prepared analogues of two bioactive stilbenes, a pawhuskin and a schweinfurthin, where a 1,2,3-triazole ring formally replaces the stilbene double bond. The new schweinfurthin analogue (23) has been tested for anti-proliferative activity against 60 cell lines, and shows a strong correlation of bioactivity when compared to the compound that inspired its synthesis (22). Copyright © 2022. Published by Elsevier Ltd.

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External Sources

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  2. DOI: 10.1016/j.bmcl.2022.128980
  3. PMID: 36096344
  4. PII : S0960-894X(22)00456-5

Library Notes

  1. Fiscal Year: FY2022-2023
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