2. Academic Validation
  3. (2S,2'R)-analogue of LG190178 is a major active isomer

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

  • Bioorg Med Chem Lett. 2008 Jan 1;18(1):120-3. doi: 10.1016/j.bmcl.2007.11.007.
Wataru Hakamata 1,  Yukiko Sato,  Haruhiro Okuda,  Shinobu Honzawa,  Nozomi Saito,  Seishi Kishimoto,  Atsushi Yamashita,  Takayuki Sugiura,  Atsushi Kittaka,  Masaaki Kurihara
Affiliations

Affiliation

  • 1 Division of Organic Chemistry, National Institute of Health Sciences, Kamiyoga, Setagaya-ku, Tokyo 158-8501, Japan.
PMID: 18054230 DOI: 10.1016/j.bmcl.2007.11.007
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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