2-Phenyl-1-[4-(2-piperidine-1-yl-ethoxy)benzyl]-1H-benzimidazoles as ligands for the estrogen receptor: Synthesis and pharmacological evaluation |
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Authors: | Sandra Dettmann Katrin Szymanowitz Anja Wellner Anke Schiedel Christa E Müller Ronald Gust |
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Institution: | 1. Institut für Pharmazie, Freie Universität Berlin, Königin-Luise-Str. 2+4, D-14195 Berlin, Germany;2. Pharmaceutical Institute, Pharmaceutical Chemistry I, University of Bonn, D-53115 Bonn, Germany;3. Institut für Pharmazie, Universität Innsbruck, Innrain 52, A-6020 Innsbruck, Austria |
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Abstract: | 2-Phenyl-1H-benzimidazoles 7a–e were synthesized and tested for gene activation on ERα-positive MCF-7 breast cancer cells, stably transfected with the reporter plasmid EREwtcluc (MCF-7-2a cells). None of the compounds showed agonistic properties, but they antagonized dependent on hydroxyl groups at the benzimidazole core (5- or 6-OH) and at the aromatic ring in the 2-position (4-OH) in high concentrations the gene activation induced by estradiol (E2, 1 nM). All compounds exhibited significant antiproliferative properties on MCF-7 cells but they were inactive against hormone independent, ER negative MDA-MB-231 cells. |
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