title: Synthesis and biological activity of 3-N-substituted estrogen derivatives as breast cancer agents.
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 = 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).
authors.affiliation: College of Pharmacy and Pharmaceutical Sciences, Florida A&M University, Tallahassee, Florida 32307, USA.
authors.forename: Zhongliang
authors.initials: Z
authors.lastname: Wan
authors.forename: Musiliyu A
authors.initials: MA
authors.lastname: Musa
authors.forename: Patrick
authors.initials: P
authors.lastname: Joseph
authors.forename: John S
authors.initials: JS
authors.lastname: Cooperwood
mesh_terms: D001943:Breast Neoplasms / Q000473:pathology*; D045744:Cell Line, Tumor; D004967:Estrogens / Q000494:pharmacology*; D005260:Female; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D021241:Spectrometry, Mass, Electrospray Ionization
chemical_list: D004967:Estrogens