Lead identification of a potent benzopyranone selective estrogen receptor modulator

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

Index: 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

Full Text: HTML

Citation Number: 31

Abstract

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.