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Synthesis and Evaluation of Estradiol Derivatives as Anti-Breast Cancer Agents. 2010
John S Cooperwood, and
Jesse Edwards, and
Musiliyu Musa, and
Devora Simmons, and
Abdul D Mian, and
Kwon-Kyun Park, and
Zhongliang Wan
Florida A&M University College of Pharmacy and Pharmaceutical Sciences, Tallahassee, Florida 32307, USA; Tel: 1-850-599-3110; fax: 1-850-599-3323.
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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