An efficient synthesis of argifin: a natural product chitinase inhibitor with chemotherapeutic potential

Mark J. Dixon, Ole A. Andersen, Daan M. F. van Aalten, Ian M. Eggleston

    Research output: Contribution to journalArticle

    31 Citations (Scopus)

    Abstract

    The first synthesis of the cyclopentapeptide family 18 chitinase inhibitor argifin has been achieved by a combination of solid phase and solution chemistry. Synthetic argifin is a nanomolar inhibitor of chitinase B1 from Aspergillus fumigatus and the high-resolution X-ray structure of the synthesized material in complex with the same enzyme is identical to that previously obtained for the natural product.

    Original languageEnglish
    Pages (from-to)4717-4721
    Number of pages5
    JournalBioorganic & Medicinal Chemistry Letters
    Volume15
    Issue number21
    DOIs
    Publication statusPublished - 1 Nov 2005

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