Structural development of non-secosteroidal vitamin D receptor (VDR) ligands without any asymmetric carbon

[Display omitted] 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 ago...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2018-12, Vol.26 (23-24), p.6146-6152
Main Authors: Misawa, Takashi, Tsuji, Genichiro, Takahashi, Takeo, Ochiai, Eiji, Takagi, Ken-ichiro, Horie, Kyohei, Kakuda, Shinji, Takimoto-Kamimura, Midori, Kurihara, Masaaki, Demizu, Yosuke
Format: Article
Language:English
Subjects:
Asymmetric carbon
Biphenyl Compounds - chemical synthesis
Biphenyl Compounds - chemistry
Biphenyl Compounds - pharmacology
Docking study
Dose-Response Relationship, Drug
Humans
Ligands
Models, Molecular
Molecular Structure
Non-secosteroid
Receptors, Calcitriol - agonists
Structure-Activity Relationship
Vitamin D receptor
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Summary:[Display omitted] 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.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2018.11.008