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. 2018 Dec 15;26(23-24):6146-6152.
doi: 10.1016/j.bmc.2018.11.008. Epub 2018 Nov 9.

Structural Development of Non-Secosteroidal Vitamin D Receptor (VDR) Ligands Without Any Asymmetric Carbon

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Structural Development of Non-Secosteroidal Vitamin D Receptor (VDR) Ligands Without Any Asymmetric Carbon

Takashi Misawa et al. Bioorg Med Chem. .

Abstract

Non-secosteroidal VDR ligands without any assymmetric carbon were designed and synthesized based on the structure of the previously reported non-secosteroidal VDR agonist LG190178. The VDR-agonistic activity of all synthesized compounds was evaluated, and 7b emerged as a potent agonist activity with an EC50 value of 9.26 nM. Moreover, a docking simulation analysis was also performed to determine the binding mode of 7b with VDR-LBD.

Keywords: Asymmetric carbon; Docking study; Non-secosteroid; Vitamin D receptor.

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