Synthesis and biological evaluation of (+)-neopeltolide analogues: Importance of the oxazole-containing side chain

Haruhiko Fuwa, Takuma Noguchi, Masato Kawakami, Makoto Sasaki

    Research output: Contribution to journalArticle

    21 Citations (Scopus)

    Abstract

    We describe the synthesis and biological evaluation of (+)-neopeltolide analogues with structural modifications in the oxazole-containing side chain. Evaluation of the antiproliferative activity of newly synthesized analogues against A549 human lung adenocarcinoma cells and PANC-1 human pancreatic carcinoma cells have shown that the C19-C20 and C26-C27 double bonds within the oxazole-containing side chain and the terminal methyl carbamate group are essential for potent activity.

    Original languageEnglish
    Pages (from-to)2415-2419
    Number of pages5
    JournalBioorganic and Medicinal Chemistry Letters
    Volume24
    Issue number11
    DOIs
    Publication statusPublished - 2014 Jun 1

    Keywords

    • Antiproliferative activity
    • Macrolides
    • Marine natural products
    • Structure-activity relationships
    • Suzuki-Miyaura coupling

    ASJC Scopus subject areas

    • Biochemistry
    • Molecular Medicine
    • Molecular Biology
    • Pharmaceutical Science
    • Drug Discovery
    • Clinical Biochemistry
    • Organic Chemistry

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