Lead identification of a potent benzopyranone selective estrogen receptor modulator

Bioorg Med Chem Lett. 2004 Jul 5;14(13):3407-10. doi: 10.1016/j.bmcl.2004.04.081.

Jeffrey A McKie ¹, Shripad S Bhagwat, Helen Brady, Mary Doubleday, Leah Gayo, Mathew Hickman, Ravi K Jalluri, Sak Khammungkhune, Adam Kois, Deborah Mortensen, Normand Richard, John Sapienza, Graziella Shevlin, Bernd Stein, May Sutherland

Affiliations

Affiliation

1 Medicinal Chemistry, Celgene, San Diego, CA 92121, USA. [email protected]

PMID: 15177442 DOI: 10.1016/j.bmcl.2004.04.081

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.

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