3,5-Disubstituted pyranone analogues of highly antifungally active furanones: Conversion of biological effect from antifungal to cytostatic

作者：Schiller Radan; Tichotova Lucie; Pavlik Jan; Buchta Vladimir; Melichar Bohuslav; Votruba Ivan; Kunes Jiri; Spulak Marcel; Pour Milan^*

来源：Bioorganic & Medicinal Chemistry Letters, 2010, 20(24): 7358-7360.

DOI：10.1016/j.bmcl.2010.10.052

• Pyranone
• Synthesis
• Screening
• Antifungal
• Cytostatic

A series of 3-aryl-5-acyloxymethyl-5,6-dihydro-2H-pyran-2-ones, related to highly antifungally active butenolides, was synthesized via cyclization of substituted delta-hydroxy acids as the key step, and evaluated for their in vitro antifungal activity and cytostatic activity. While the extension of the furanone ring to pyranone led to a complete loss of the antifungal effect, some of the compounds displayed promising effect against several cell lines, including the resistant colorectal carcinoma cells.

• 出版日期2010-12-15