Journal of medicinal chemistry

Structure-activity relationship study to understand the estrogen receptor-dependent gene activation of aryl-and alkyl-substituted 1 H-imidazoles

T Wiglenda, R Gust

Index: Wiglenda, Thomas; Gust, Ronald Journal of Medicinal Chemistry, 2007 , vol. 50, # 7 p. 1475 - 1484

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Citation Number: 75

Abstract

A series of C5-substituted 1, 2, 4-triaryl-1 H-imidazoles was synthesized. Their gene- activating properties were determined on estrogen receptor alpha positive MCF-7 breast cancer cells, stably transfected with the plasmid EREwtcluc (MCF-7-2a cells). The influence of 4-OH and 2-Cl substituents on the phenyl rings as well as the significance of a methyl, ethyl, or phenyl group at C5 on the estrogen receptor binding and the resulting gene ...