Lead identification of a potent benzopyranone selective estrogen receptor modulator

…, D Mortensen, N Richard, J Sapienza, G Shevlin…

文献索引：McKie, Jeffrey A.; Bhagwat, Shripad S.; Brady, Helen; Doubleday, Mary; Gayo, Leah; Hickman, Mathew; Jalluri, Ravi K.; Khammungkhune, Sak; Kois, Adam; Mortensen, Deborah; Richard, Normand; Sapienza, John; Shevlin, Graziella; Stein, Bernd; Sutherland, May Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 13 p. 3407 - 3410

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被引用次数: 31

摘要

Starting from a phenol screening hit (6), three series of benzopyranone selective estrogen receptor modulators (SERMs) have been designed, synthesized, and analyzed for both estrogen receptor alpha binding affinity and in vitro activity in two cell assays. The lead compound identified, SP500263 (13), was more potent than raloxifene and tamoxifen in a cell-based assay measuring inhibition of interleukin-6 release.