In uterotrophic assay newly synthesized compounds 2–5 showed a complete loss of estrogenic activity, whereas derivatives 2–4 exhibited slight, and compound 5 higher antiestrogenic effects. On the other hand, anti-aromatase assay showed that compounds 2, 3, and 4 possess inhibition potency, although lower than standard aromatase inhibitor aminoglutethimide. Cytotoxicity of compounds 2–5, estradiol and tamoxifen against several human tumor or healthy cell lines (MCF-7, MDA-MB-231, HT-29, and MRC-5) was evaluated after short-time treatment.