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Structural development of non-secosteroidal vitamin D receptor (VDR) ligands without any asymmetric carbon |
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| Authors: | Takashi Misawa Genichiro Tsuji Takeo Takahashi Eiji Ochiai Ken-ichiro Takagi Kyohei Horie Shinji Kakuda Midori Takimoto-Kamimura Masaaki Kurihara Yosuke Demizu |
| Institution: | 1. Division of Organic Chemistry, National Institute of Health Sciences, 3-25-26 Tonomachi, Kawasaki-ku, Kawasaki-shi, Kanagawa 210-9501, Japan;2. Teijin Institute for Bio-Medical Research, Teijin Pharma Ltd., Tokyo 191-8512, Japan;3. Department of Pharmaceutical Sciences, International University of Health and Welfare, 2600-1 Kitakanemaru, Otawara City, Tochigi 324-8501, Japan |
| 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: | Vitamin D receptor Non-secosteroid Asymmetric carbon Docking study |
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