Design and synthesis of aryl diphenolic azoles as potent and selective estrogen receptor-beta ligands.

@article{Malamas2004DesignAS,
  title={Design and synthesis of aryl diphenolic azoles as potent and selective estrogen receptor-beta ligands.},
  author={Michael S Malamas and Eric S. Manas and Robert E McDevitt and Iwan Gunawan and Zhang Bao Xu and Michael D Collini and Chris P Miller and Tam Q. Dinh and R. C. A. Henderson and J. S. Keith and Heather A. Harris},
  journal={Journal of medicinal chemistry},
  year={2004},
  volume={47 21},
  pages={5021-40}
}
New diphenolic azoles as highly selective estrogen receptor-beta agonists are reported. The more potent and selective analogues of these series have comparable binding affinities for ERbeta as the natural ligand 17beta-estradiol but are >100-fold selective over ERalpha. Our design strategy not only followed a traditional SAR approach but also was supported by X-ray structures of ERbeta cocrystallized with various ligands as well as molecular modeling studies. These strategies enabled us to take… CONTINUE READING