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 nat ural 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 mu M, chalcones inh ibited ovarian cancer cell proliferation and [H-3]oestradiol ([H-3]E2) binding to type II EBS. Considering the structure-related variation i n IC50 (concentration resulting in a 50% inhibition of cell growth) an d Di(50) (concentration resulting in a 50% displacement of [H-3]E2 bou nd to type II EBS), it appeared that the presence of an alpha-beta dou ble bond, the hydroxylation in 3 or 2 of ring B and the absence of a p renyl group were important to both the antiproliferative and binding a ctivity. Structure-related variations in IC50 and Di(50) were signific antly concordant (Fisher's exact test: P = 0.0291), suggesting that-th ere may be a type II EBS-mediated mechanism for chalcone antiprolifera tive activity. Our data indicate that chalcones could be considered as potential new anticancer drugs.