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

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...

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Bibliographic Details
Published inLetters in drug design & discovery Vol. 7; no. 6; p. 389
Main Authors Cooperwood, John S, Edwards, Jesse, Musa, Musiliyu, Simmons, Devora, Mian, Abdul D, Park, Kwon-Kyun, Wan, Zhongliang
Format Journal Article
LanguageEnglish
Published United Arab Emirates 01.07.2010
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Summary: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.
ISSN:1570-1808
DOI:10.2174/157018010791306551