(2S,2'R)-analogue of LG190178 is a major active isomer.
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.
Division of Organic Chemistry, National Institute of Health Sciences, Kamiyoga, Setagaya-ku, Tokyo 158-8501, Japan.
Wataru
W
Hakamata
Yukiko
Y
Sato
Haruhiro
H
Okuda
Shinobu
S
Honzawa
Nozomi
N
Saito
Seishi
S
Kishimoto
Atsushi
A
Yamashita
Takayuki
T
Sugiura
Atsushi
A
Kittaka
Masaaki
M
Kurihara
D001713:Biphenyl Compounds / Q000737:chemistry* / Q000494:pharmacology*; D002117:Calcitriol / Q000031:analogs & derivatives* / Q000737:chemistry / Q000378:metabolism; D015195:Drug Design; D008024:Ligands; D008958:Models, Molecular; D018167:Receptors, Calcitriol / Q000737:chemistry / Q000378:metabolism*; D013237:Stereoisomerism
D001713:Biphenyl Compounds; D008024:Ligands; D018167:Receptors, Calcitriol; C526404:YR301; D002117:Calcitriol