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.
Keywords: Estradiol, Estrogen Receptors, SERMs, MCF-7 cells, 4-hydroxytamoxifen, Breast cancer
Letters in Drug Design & Discovery
Title: Synthesis and Evaluation of Estradiol Derivatives as Anti-Breast Cancer Agents
Volume: 7 Issue: 6
Author(s): John S. Cooperwood, Jesse Edwards, Musiliyu Musa, Devora Simmons, Abdul D. Mian, Kwon-kyun Park and Zhongliang Wan
Affiliation:
Keywords: Estradiol, Estrogen Receptors, SERMs, MCF-7 cells, 4-hydroxytamoxifen, Breast cancer
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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Cite this article as:
S. Cooperwood John, Edwards Jesse, Musa Musiliyu, Simmons Devora, D. Mian Abdul, Park Kwon-kyun and Wan Zhongliang, Synthesis and Evaluation of Estradiol Derivatives as Anti-Breast Cancer Agents, Letters in Drug Design & Discovery 2010; 7 (6) . https://dx.doi.org/10.2174/157018010791306551
DOI https://dx.doi.org/10.2174/157018010791306551 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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