Synthesis and biological evaluation of steroidal derivatives bearing a small ring as vitamin D receptor agonists.

@article{Arichi2017SynthesisAB,
  title={Synthesis and biological evaluation of steroidal derivatives bearing a small ring as vitamin D receptor agonists.},
  author={Norihito Arichi and Shinichi Fujiwara and Michiyasu Ishizawa and Makoto Makishima and Duy H Hua and Ken-ichi Yamada and Yousuke Yamaoka and Kiyosei Takasu},
  journal={Bioorganic & medicinal chemistry letters},
  year={2017},
  volume={27 15},
  pages={3408-3411}
}
A novel series of 3-ketolithocholic acid derivatives as well as estrone derivatives bearing a small ring for the conformational fixation of the side chain were synthesized by using a catalytic [2+2] cycloaddition and a ring-contraction rearrangement. The steroidal derivatives were evaluated for transcriptional activation of vitamin D receptor by luciferase… CONTINUE READING