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Synthesis and Biological Activity of 3-N-Substituted Estrogen Derivatives as Breast Cancer Agents

[ Vol. 13 , Issue. 9 ]


Zhongliang Wan, Musiliyu A Musa, Patrick Joseph and John S. Cooperwood   Pages 1381 - 1388 ( 8 )


3-N-substituted-estrogen derivatives were synthesized and characterized. Their antiproliferative activities against human ER (+) MCF-7 (Breast), ER (-) MDA-MB-231 (breast) and Ishikawa (endometrial) cancer cell lines were determined after 72 hours drug exposure employing CellTiter-Glo assay at concentrations ranging from (0.01-100,000 nM). The antiproliferative activities of these compounds were compared to tamoxifen (TAM), 4-hydroxytamoxifen (4-OHT, active metabolite of tamoxifen) and raloxifene (RAL). In vitro results indicated that compound 5 (IC50 = 12µM) displayed comparable antiproliferative activity against MDA-MB 231 cell line; while compounds 6, 7 and 13 (IC50 = 12µM) displayed higher activity against MCF-7 and Ishikawa cell lines, in comparison to TAM activity (19-33µM).


3-N-substituted estrogen derivatives, antiproliferative activity, breast cancer.


College of Pharmacy and Pharmaceutical Sciences, Florida A&M University, Tallahassee, Florida 32307, USA.

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