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 IC(50) values. The IC(50)s were correlated with structures using molecular modeling.

中文翻译：

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作为抗乳腺癌药物的雌二醇衍生物的合成与评价

3-N-烷氧基雌二醇衍生物被合成、表征和测试在MCF-7人乳腺癌细胞中的活性。在这些化合物中，发现二异丙基和哌啶衍生物比基于 IC(50) 值的他莫昔芬的活性代谢物 4-羟基三苯氧胺 (HO-Tam) 更具活性。IC(50)s 与使用分子建模的结构相关。