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

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 IC(50) values. The IC(50)s were correlated with structures using molecular modeling.

SUBMITTER: Cooperwood JS

PROVIDER: S-EPMC2882686 | biostudies-literature | 2010 Jul

REPOSITORIES: biostudies-literature

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

Cooperwood John S JS Edwards Jesse J Musa Musiliyu M Simmons Devora D Mian Abdul D AD Park Kwon-Kyun KK Wan Zhongliang Z

Letters in drug design & discovery 20100701 6

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. ...[more]

PMID: 20543998

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