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Bioorg Med Chem Lett. 2008 Jan 1;18(1):120-3. Epub 2007 Nov 5.

(2S,2'R)-analogue of LG190178 is a major active isomer.

Author information

1
Division of Organic Chemistry, National Institute of Health Sciences, Kamiyoga, Setagaya-ku, Tokyo 158-8501, Japan.

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.

PMID:
18054230
DOI:
10.1016/j.bmcl.2007.11.007
[Indexed for MEDLINE]

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