Abstract. In this study, we investigated the antiproliferative activity of the isoflavones daidzein and genistein in three breast cancer cell lines with different patterns of estrogen receptor (ER) and c-erbB-2 protein expression (ERα-positive MCF-7 cells, c-erbB-2-positive SK-BR-3 cells and ERα/c-erbB-2-positive ZR-75-1). After treatment at various concentrations (1-200 µM for 72 h), the effect of daidzein and genistein on the proliferation of different cell types varied; these effects were found to be associated with ERα and c-erbB-2 expression. Daidzein and genistein exhibited biphasic effects (stimulatory or inhibitory) on proliferation and ERα expression in MCF-7 cells. Although 1 µM daidzein significantly stimulated cell growth, ERα expression was unaffected. However, genistein showed marked increases in proliferation and ERα expression after exposure to <10 µM genistein. Notably, the inhibition of cell proliferation by 200 µM genistein was greater compared to that by daidzein at the same concentration. Daidzein and genistein significantly inhibited proliferation of SK-BR-3 and ZR-75-1 cells in a dose-dependent manner. In addition, ERα and c-erbB-2 expression was reduced by daidzein and genistein in both SK-BR-3 and ZR-75-1 cells in a dose-dependent manner. However, the effect of genistein was greater compared to that of daidzein. In conclusion, the isoflavones daidzein and genistein showed anti-breast cancer activity, which was associated with expression of the ERα and c-erbB-2 receptors.