Synthesis and structure-activity relationship of 3-arylbenzoxazines as selective estrogen receptor beta agonists.

@article{Yang2004SynthesisAS,
  title={Synthesis and structure-activity relationship of 3-arylbenzoxazines as selective estrogen receptor beta agonists.},
  author={W P Yang and Yufeng Wang and Zhengping Ma and Rajasree Golla and Terry R. Stouch and Ramakrishna Seethala and Susan E. Johnson and Rong Zhou and Timur G{\"u}ng{\"o}r and Jean H M Feyen and John K Dickson},
  journal={Bioorganic & medicinal chemistry letters},
  year={2004},
  volume={14 9},
  pages={2327-30}
}
A series of 3-aryl-7-hydroxybenzoxazine analogues have been prepared and evaluated as ligands for the two estrogen receptor subtypes (ERalpha and ERbeta). From the radioligand binding assay, compounds with more than a 10-fold binding selectivity toward the ERbeta subtype have been identified. These compounds have also been shown to be potent full agonists in the functional assay by activation of ERE promoted transcription, with the best compound being 20-fold more potent than genistein.