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

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Hakamata W,Sato Y,Okuda H,Honzawa S,Saito N,Kishimoto S,Yamashita A,Sugiura T,Kittaka A,Kurihara M

doi

10.1016/j.bmcl.2007.11.007

subject

Has Abstract

pub_date

2008-01-01 00:00:00

pages

120-3

issue

1

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(07)01315-7

journal_volume

18

pub_type

杂志文章

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