Synthesis, biological evaluation, structural–activity relationship, and docking study for a series of benzoxepin-derived estrogen receptor modulators

…, AJS Knox, N Artemenko, G Golfis, DM Zisterer…

Index: Barrett, Irene; Meegan, Mary J.; Hughes, Rosario B.; Carr, Miriam; Knox, Andrew J.S.; Artemenko, Natalia; Golfis, Georgia; Zisterer, Daniela M.; Lloyd, David G. Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 21 p. 9554 - 9573

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Citation Number: 34

Abstract

The estrogen receptors ERα and ERβ are recognized as important pharmaceutical targets for a variety of diseases including osteoporosis and breast cancer. A series of novel benzoxepin-derived compounds are described as potent selective modulators of the human estrogen receptor modulators (SERMs). We report the antiproliferative effects of these compounds on human MCF-7 breast tumor cells. These heterocyclic compounds contain ...