Crystal structure and potent antifungal activity of synthetic homoisoflavanone analogues

A series of seven homoisoflavanone analogues (1-7) were synthesized previously from the corresponding substituted phenols via chroman-4-one in three steps. These analogues were evaluated for their antifungal activity against Candida albicans. Compound 3, (E)-5,7-dimethoxy-3-benzylidene-4-chromanone, showed the highest activity (MIC50 = 25 μM), which is better than the reference drug clotrimazole (MIC50 = 42 μM). The X-ray structure of this compound is also reported. The cytotoxicity of the compounds was also investigated against Chinese Hamster Ovarian (CHO) cells in an MTT assay and the data shows variable results but in general much less toxicity than the control drug emetine.