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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Published in | Letters in drug design & discovery Vol. 7; no. 6; p. 389 |
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Main Authors | , , , , , , |
Format | Journal Article |
Language | English |
Published |
United Arab Emirates
01.07.2010
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Online Access | Get more information |
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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. |
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ISSN: | 1570-1808 |
DOI: | 10.2174/157018010791306551 |