Bioorganic and Medicinal Chemistry Letters p. 3407 - 3410 (2004)
Update date:2022-08-05
Topics:
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
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.
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