Synthesis of 7α-substituted derivatives of 17β-estradiol

XR Jiang, JW Sowell, BT Zhu

Index: Jiang, Xiang-Rong; Walter Sowell; Zhu, Bao Ting Steroids, 2006 , vol. 71, # 5 p. 334 - 342

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Citation Number: 19

Abstract

Estrogen receptor (ER) pure antagonists such as ICI-182,780 (fulvestrant) are effective alternatives to tamoxifen (an ER antagonist/weak partial agonist) in the treatment of postmenopausal, receptor-positive human breast cancers. Structurally, these pure antagonists contain the basic core structure of 17β-estradiol (E2) with a long side chain attached to its C-7α position. We explored and compared in this study various synthetic ...