3-N-alkyloxyestradiol derivatives were synthesized, characterized and tested for activity in MCF-7 human breast cancer cells. Among the compounds, the diisopropyl and piperidinyl derivatives were found to be more active than 4-hydroxytamoxifen (HO-Tam), the active metabolite of tamoxifen based upon IC50 values. The IC50s were correlated with structures using molecular modeling.
Keywords: Estradiol, Estrogen Receptors, SERMs, MCF-7 cells, 4-hydroxytamoxifen, Breast cancer
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