Bioorganic and Medicinal Chemistry Letters
Bioorganic and Medicinal Chemistry Letters
5 years ago

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

Synthesis and biological evaluation of steroidal derivatives bearing a small ring as vitamin D receptor agonists
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 reporter assays. Among them, two estrone derivatives showed a higher efficacy of the transactivation of vitamin D receptor than 3-ketolithocholic acid, and the small ring moieties were found to be important for the efficacy.

Publisher URL: www.sciencedirect.com/science

DOI: S0960894X17306017

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