Lead identification of a potent benzopyranone selective estrogen receptor modulator.

@article{McKie2004LeadIO,
  title={Lead identification of a potent benzopyranone selective estrogen receptor modulator.},
  author={Jeffrey A. McKie and Shripad S. Bhagwat and Helen Brady and M. R. Doubleday and Leah Gayo and Matthew Hickman and Ravi K Jalluri and Sak Khammungkhune and Adam Kois and Deborah J Mortensen and Normand Richard and John Sapienza and Graziella I Shevlin and Bernd Stein and May S Kung Sutherland},
  journal={Bioorganic & medicinal chemistry letters},
  year={2004},
  volume={14 13},
  pages={3407-10}
}
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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