Influence of Chlorine or Fluorine Substitution on the Estrogenic Properties of 1-Alkyl-2, 3, 5-tris (4-hydroxyphenyl)-1 H-pyrroles

…, M Strauss, A Schäfer, G Wolber, R Gust

Index: Schaefer, Anja; Wellner, Anja; Strauss, Martin; Schaefer, Andreas; Wolber, Gerhard; Gust, Ronald Journal of Medicinal Chemistry, 2012 , vol. 55, # 22 p. 9607 - 9618

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Citation Number: 8

Abstract

In continuation of our previous work, several 1-alkyl-2, 3, 5-tris (4-hydroxyphenyl) aryl-1 H- pyrroles with chlorine or fluorine substituents in the aryl residues were synthesized and tested for estrogen receptor (ER) binding at isolated ERα/ERβ receptors (HAP assay) and in transactivation assays using ERα-positive MCF-7/2a as well as U2-OS/ERα and U2-OS/ERβ cells. In the competition experiment at ERα the compounds displayed very high relative ...