Synthesis and Evaluation of Estradiol Derivatives as Anti-Breast Cancer Agents
雌二醇衍生物的合成及作为抗乳腺癌药物的评价
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作者：John S Cooperwood, Jesse Edwards, Musiliyu Musa, Devora Simmons, Abdul D Mian, Kwon-Kyun Park, Zhongliang Wan
Abstract
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.
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