Počet záznamů: 1

Synthesis and biological activity of desmethoxy analogues of coruscanone A

  1. 1.
    0367571 - UOCHB-X 2012 RIV GB eng J - Článek v odborném periodiku
    Tichotová, L. - Matoušová, E. - Špulák, M. - Kuneš, J. - Votruba, Ivan - Buchta, V. - Pour, M.
    Synthesis and biological activity of desmethoxy analogues of coruscanone A.
    Bioorganic and Medicinal Chemistry Letters. Roč. 21, č. 20 (2011), s. 6062-6066 ISSN 0960-894X
    Grant CEP: GA MŠk 1M0508
    Grant ostatní:GA ČR(CZ) GAP207/10/2048
    Výzkumný záměr: CEZ:AV0Z40550506
    Klíčová slova: cyclopentenediones * knoevenagel * Lewis acid * antifungal * cytotoxicity
    Kód oboru RIV: CC - Organická chemie
    Impakt faktor: 2.554, rok: 2011

    A series of simple desmethoxy analogues of coruscanone A was prepared via a novel version of Ti(iPrO)4-mediated Knoevenagel condensation of cyclopentenedione with substituted benzaldehydes and cinnamic aldehydes, and the compounds were evaluated for antifungal activity and cytotoxicity. The most potent 2-benzylidenecyclopent-4-ene-1,3-dione possessed antifungal effect comparable to coruscanone A and a somewhat broader spectrum of activity against Candida species. The compound was also superior to fluconazole against several non-albicans Candida sp. Evaluation of the ability of the compound to influence cell proliferation using two different assays showed that 2-benzylidenecyclopent- 4-ene-1,3-dione has lower cytotoxicity compared to the natural product.
    Trvalý link: http://hdl.handle.net/11104/0202201