Enhanced estrogen receptor beta (ERβ) selectivity of fluorinated carborane-containing ER modulators.

@article{Ohta2013EnhancedER,
  title={Enhanced estrogen receptor beta (ERβ) selectivity of fluorinated carborane-containing ER modulators.},
  author={Kiminori Ohta and Takumi Ogawa and Asako Kaise and Yasuyuki Endo},
  journal={Bioorganic & medicinal chemistry letters},
  year={2013},
  volume={23 24},
  pages={6555-8}
}
We previously showed that fluorination of the carborane-containing selective estrogen receptor modulator (SERM) BE360 altered the agonist/antagonist activity balance and the estrogen receptor (ER) α/β subtype selectivity. Here, we designed and synthesized a series of fluorinated carboranyl phenols as candidate ERβ-selective ligands. Introduction of a fluorine atom onto the carborane cage commonly reduced the binding affinity for ERα, to an extent that depended on the other substituents present… CONTINUE READING
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