Torsionally and hydrophobically modified 2, 3-diarylindenes as estrogen-receptor ligands

…, SR Wilson, JA Katzenellenbogen

Index: Anstead, Gregory M.; Peterson, Chad S.; Pinney, Kevin G.; Wilson, Scott R.; Katzenellenbogen, John A. Journal of Medicinal Chemistry, 1990 , vol. 33, # 10 p. 2726 - 2734

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Citation Number: 18

Abstract

2, 3-Diarylindenes are ligands for the estrogen receptor which display intrinsic fluorescence. In order to optimize the receptor binding affinity of these compounds while preserving their desirable fluorescence properties, a series of torsionally modified analogues were prepared. A fluorine or methyl group was introduced on either of the two phenyl substituents ortho to their attachment site to the indene nucleus, in order to increase the out-of-plane twist of ...