Lead identification of a potent benzopyranone selective estrog...

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Lead identification of a potent benzopyranone selective estrogen receptor modulator.
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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.
McKie JA, Bhagwat SS, Brady H, Doubleday M, Gayo L, Hickman M, Jalluri RK, Khammungkhune S, Kois A, Mortensen D, Richard N, Sapienza J, Shevlin G, Stein B, and Sutherland M
Bioorganic & medicinal chemistry letters 14(13):3407-10, 2004 Jul 5 - Who cited this? | PubMed ID: 15177442 | Fulltext
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