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

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

Volume: 13 Issue: 9

Author(s): Zhongliang Wan, Musiliyu A Musa, Patrick Joseph and John S. Cooperwood

Affiliation:

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

Abstract: 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).

Cite this article as:

Wan Zhongliang, Musa A Musiliyu, Joseph Patrick and Cooperwood S. John, Synthesis and Biological Activity of 3-N-Substituted Estrogen Derivatives as Breast Cancer Agents, Mini-Reviews in Medicinal Chemistry 2013; 13 (9) . https://dx.doi.org/10.2174/1389557511313090012