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

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.

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