Synthesis and Evaluation of Estradiol Derivatives as Anti-Breast Cancer Agents

Author(s): John S. Cooperwood, Jesse Edwards, Musiliyu Musa, Devora Simmons, Abdul D. Mian, Kwon-kyun Park, Zhongliang Wan.

Journal Name: Letters in Drug Design & Discovery

Volume 7 , Issue 6 , 2010

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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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Article Details

Year: 2010
Page: [389 - 394]
Pages: 6
DOI: 10.2174/157018010791306551
Price: $65

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