280138-19-4Relevant academic research and scientific papers
Lead identification of a potent benzopyranone selective estrogen receptor modulator
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
, p. 3407 - 3410 (2004)
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.
Use of benzopyranones for treating or preventing a primary brain cancer or a brain metastasis
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, (2008/06/13)
This invention relates to methods for using benzopyranones, or their pharaceutically acceptable salts, for treating or preventing a primary brain cancer or a brain metastasis. The benzopyranones have the formula: wherein R1, R2, Rsu
Compounds and methods for modulation of estrogen receptors
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, (2008/06/13)
Compounds that modulate gene expression through the estrogen receptor (ER) are disclosed having the following structure, as well as pharmaceutical compositions containing the same: wherein R1, R2, R3, n and p are as define
