Synthesis and biological evaluation of guanylhydrazone coactivator binding inhibitors for the estrogen receptor

…, JR Gunther, KE Carlson, JA Katzenellenbogen

Index: LaFrate, Andrew L.; Gunther, Jillian R.; Carlson, Kathryn E.; Katzenellenbogen, John A. Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 23 p. 10075 - 10084

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Citation Number: 49

Abstract

Most patients with hormone-responsive breast cancer eventually develop resistance to traditional antiestrogens such as tamoxifen, and this has become a major obstacle in their treatment. We prepared and characterized the activity of a series of 16 guanylhydrazone small molecules that are designed to block estrogen receptor (ER) activity through a non- traditional mechanism, by directly interfering with coactivator binding to agonist-liganded ...