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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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2882686 | PMC |
| http://dx.doi.org/10.2174/157018010791306551 | DOI Listing |
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