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Natural and synthetic furanones with anticancer activity

par Cimmino, Alessio;Evidente, Antonio;Scafato, Patrizia;Mathieu, Véronique ;Ingels, Aude ;D'Amico, Wanda;Pisani, Laura;Maddau, Lucia;Superchi, Stefano;Kiss, Robert
Référence Natural Product Communications, 11, 10, page (1471-1474)
Publication Publié, 2016

Article révisé par les pairs

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Résumé :

This paper describes the enantioselective synthesis of analogues of sapinofuranones a and B, namely 5-substitutes dihydro- and 5H-furan-ones, and their in vitro growth inhibitory activity against six cancer cell lines in comparison with fungal furanones such as diplofuranone A, diplobifuranylones a and B, as well as (S, S)-enantiomer of sapinofuranone B. The compounds under study displayed weak if any in vitro growth inhibitory activity against the analysed cancer cell lines. However, it seems that among dihydro- and 5H-furan-ones bearing a 1-hydroxypentyl side chain, the stereochemistry of the furanone ring and that of hydroxylated methine could modify the in vitro growth activity of these compounds. The natural furanones that showed a different unsaturated chain at C-4 or rearranged into a dihydrofuran ring appeared to be inactive in terms of growth inhibitory activity, e.g. displaying growth inhibitory concentration at 50% (GI50) > 100 μM in all six cancer cell lines analysed.