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- ISSN: 1570-1808
- E-ISSN: 1875-628X
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Synthesis and Evaluation of Estradiol Derivatives as Anti-Breast Cancer Agents
- Source: Letters in Drug Design & Discovery, Volume 7, Issue 6, Jul 2010, p. 389 - 394
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- 01 Jul 2010
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 IC50 values. The IC50s were correlated with structures using molecular modeling.
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