Synthesis of novel estrogen receptor antagonists using metal-catalyzed coupling reactions and characterization of their biological activity

XR Jiang, P Wang, CL Smith…

Index: Jiang, Xiang-Rong; Wang, Pan; Smith, Carolyn L.; Zhu, Bao Ting Journal of Medicinal Chemistry, 2013 , vol. 56, # 7 p. 2779 - 2790

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Citation Number: 9

Abstract

Estrogen receptor (ER) antagonists are valuable in the treatment of ER-positive human breast cancer. In this study, we designed and synthesized nine new derivatives of 17β- estradiol (E2) with a bulky side chain attached to its C-7α position, and determined their ER antagonistic activity using in vitro bioassays. Four of the derivatives showed a strong inhibition of ERα transactivation activity in a luciferase reporter assay and blocked ERα ...