Synthesis and antiestrogenic activity of diaryl thioether derivatives

D Poirier, S Auger, Y Merand, J Simard…

Index: Poirier, Donald; Auger, Serge; Merand, Yves; Simard, Jacques; Labrie, Fernand Journal of Medicinal Chemistry, 1994 , vol. 37, # 8 p. 1115 - 1125

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Citation Number: 29

Abstract

The reaction of 1, 2-diarylethanol and mercapto side chain catalyzed by ZnIz was used as a key step in the short (three to five steps) and efficient synthesis of 17 diary1 thioether derivatives. Several of these compounds contain a methyl butyl amide chain and an hydroxyaryl moiety, respectively, for antiestrogenic activity and binding affinity on estrogen receptor. No binding affinity for crude cytosolic preparation of the estrogen receptor was ...