2-Phenyl-1-[4-(2-piperidine-1-yl-ethoxy) benzyl]-1H-benzimidazoles as ligands for the estrogen receptor: Synthesis and pharmacological evaluation

S Dettmann, K Szymanowitz, A Wellner…

Index: Dettmann, Sandra; Szymanowitz, Katrin; Wellner, Anja; Schiedel, Anke; Mueller, Christa E.; Gust, Ronald Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 14 p. 4905 - 4916

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Citation Number: 9

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 ...