(2S,2'R)-analogue of LG190178 is a major active isomer |
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| Authors: | Hakamata Wataru Sato Yukiko Okuda Haruhiro Honzawa Shinobu Saito Nozomi Kishimoto Seishi Yamashita Atsushi Sugiura Takayuki Kittaka Atsushi Kurihara Masaaki |
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| Affiliation: | Division of Organic Chemistry, National Institute of Health Sciences, Kamiyoga, Setagaya-ku, Tokyo 158-8501, Japan. |
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| Abstract: | Vitamin D receptor (VDR) ligands are therapeutic agents for the treatment of psoriasis, osteoporosis, and secondary hyperparathyroidism. VDR ligands also show immense potential as therapeutic agents for autoimmune diseases and cancers of the skin, prostate, colon, and breast as well as leukemia. LG190178 is a novel non-secosteroidal ligand for VDR. We synthesized and evaluated stereoisomers of LG190178 and found that only an (2S,2'R)-analogue of LG190178 (YR301) had strong activity. |
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