Author/Authors :
Jeffrey A. McKie، نويسنده , , Shripad S. Bhagwat، نويسنده , , Helen Brady، نويسنده , , Mary Doubleday، نويسنده , , Leah Gayo، نويسنده , , Mathew Hickman، نويسنده , , Ravi K. Jalluri، نويسنده , , Sak Khammungkhune، نويسنده , , Adam Kois، نويسنده , , Deborah Mortensen، نويسنده , , Normand Richard، نويسنده , , John Sapienza، نويسنده , , Graziella Shevlin، نويسنده , , Bernd Stein، نويسنده , , May Sutherland، نويسنده ,
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.
Keywords :
e-mail: jmckie@celgene.com , Benzopyranone , Estrogen receptor modulator.* Corresponding author. Tel.: +1-858-795-4781 , fax: +1-858-795-4719
