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

Basic Information

ID: ALA4382222

Journal: Bioorg Med Chem

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

Authors: Misawa T, Tsuji G, Takahashi T, Ochiai E, Takagi KI, Horie K, Kakuda S, Takimoto-Kamimura M, Kurihara M, Demizu Y.

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.

CiteXplore: 30446437

DOI: 10.1016/j.bmc.2018.11.008

Patent ID: ┄

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