College of Pharmacy and Pharmaceutical Sciences, Florida A&M University, Tallahassee, Florida 32307, USA.
Mini Rev Med Chem. 2013 Jul;13(9):1381-8. doi: 10.2174/1389557511313090012.
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 = 12 µM) displayed comparable antiproliferative activity against MDA-MB 231 cell line; while compounds 6, 7 and 13 (IC50 = 12 µM) displayed higher activity against MCF-7 and Ishikawa cell lines, in comparison to TAM activity (19-33 µM).
合成并表征了 3-N-取代雌激素衍生物。在 72 小时药物暴露后，采用 CellTiter-Glo assay 法，在浓度范围为（0.01-100,000 nM）下，测定了这些化合物对人 ER（+）MCF-7（乳腺）、ER（-）MDA-MB-231（乳腺）和 Ishikawa（子宫内膜）癌细胞系的抗增殖活性。将这些化合物的抗增殖活性与他莫昔芬（TAM）、4-羟基他莫昔芬（4-OHT，他莫昔芬的活性代谢物）和雷洛昔芬（RAL）进行了比较。体外结果表明，化合物 5（IC50=12 μM）对 MDA-MB 231 细胞系显示出相当的抗增殖活性；而化合物 6、7 和 13（IC50=12 μM）对 MCF-7 和 Ishikawa 细胞系的活性高于 TAM 活性（19-33 μM）。
