(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.
Hakamata
Wataru
W
Division of Organic Chemistry, National Institute of Health Sciences, Kamiyoga, Setagaya-ku, Tokyo 158-8501, Japan.
Sato
Yukiko
Y
Okuda
Haruhiro
H
Honzawa
Shinobu
S
Saito
Nozomi
N
Kishimoto
Seishi
S
Yamashita
Atsushi
A
Sugiura
Takayuki
T
Kittaka
Atsushi
A
Kurihara
Masaaki
M
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