A new series of estrogen receptor modulators that display selectivity for estrogen receptor β

…, LA Orband-Miller, RG Robinett, J Shearin…

Index: Henke, Brad R.; Consler, Thomas G.; Go, Ning; Hale, Ron L.; Hohman, Dana R.; Jones, Stacey A.; Lu, Amy T.; Moore, Linda B.; Moore, John T.; Orband-Miller, Lisa A.; Robinett, R. Graham; Shearin, Jean; Spearing, Paul K.; Stewart, Eugene L.; Turnbull, Philip S.; Weaver, Susan L.; Williams, Shawn P.; Wisely, G. Bruce; Lambert, Millard H. Journal of Medicinal Chemistry, 2002 , vol. 45, # 25 p. 5492 - 5505

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Citation Number: 148

Abstract

A series of 1, 3, 5-triazine-based estrogen receptor (ER) modulators that are modestly selective for the ERβ subtype are reported. Compound 1, which displayed modest potency and selectivity for ERβ vs ERα, was identified via high-throughput screening utilizing an ERβ SPA-based binding assay. Subsequent analogue preparation resulted in the identification of compounds such as 21 and 43 that display 25-to 30-fold selectivity for ERβ with potencies ...