Effect of synthetic and naturally occurring chalcones on ovarian cancer cell growth: Structure-activity relationships

This study was carried out to determine the effect of 15 different natural and synthetic chalcones on the proliferation of both established and primary ovarian cancer cells expressing type II oestrogen binding sites (type II EBS). The binding affinity of chalcones for type II EBS was also tested. At concentrations from 0.1 to 10 μM, chalcones inhibited ovarian cancer cell proliferation and [³H]oestradiol ([³H]E2) binding to type II EBS. Considering the structure-related variation in IC₅₀ (concentration resulting in a 50% inhibition of cell growth) and Di₅₀ (concentration resulting in a 50% displacement of [³H]E2 bound to type II EBS), it appeared that the presence of an α-β double bond, the hydroxylation in 3 or 2 of ring B and the absence of a prenyl group were important, to both the antiproliferative and binding activity. Structure-related variations in IC₅₀ and Di₅₀ were significantly concordant (Fisher's exact test: P = 0.0291), suggesting that there may be a type II EBS-mediated mechanism for chalcone antiproliferative activity. Our data indicate that chalcones could be considered as potential new anticancer drugs.