Steroids

Nonsteroidal estrogens bearing acyl azide functions: potential electrophilic and photoaffinity labeling agents for the estrogen receptor

KG Pinney, KE Carlson, JA Katzenellenbogen

Index: Pinney, Kevin G,.; Carlson, Kathryn E.; Katzenellenbogen, John A. Steroids, 1992 , vol. 57, # 5 p. 222 - 232

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Citation Number: 7

Abstract

Abstract In an effort to develop novel affinity labeling agents for the estrogen receptor, we have synthesized two nonsteroidal ligands, a 1-aroyl-2-aryl tetralin system (1) and a 2-aryl-3- aroylbenzo [b] thiophene system (2). These agents, patterned after the Lilly antiestrogens trioxifene and LY 117018, respectively, embody acyl azide functions as part of a benzoyl chromophore. The acyl azide group has weak acylating activity, suitable for electrophilic ...