(2S,2′R)-Analogue of LG190178 is a major active isomer

Wataru Hakamata; Yukiko Sato; Haruhiro Okuda; Shinobu Honzawa; Nozomi Saito; Seishi Kishimoto; Atsushi Yamashita; Takayuki Sugiura; Atsushi Kittaka; Masaaki Kurihara

doi:10.1016/j.bmcl.2007.11.007

(2S,2′R)-Analogue of LG190178 is a major active isomer

Wataru Hakamata
, Yukiko Sato
, Haruhiro Okuda
, Shinobu Honzawa
, Nozomi Saito
, Seishi Kishimoto
, Atsushi Yamashita
, Takayuki Sugiura
, Atsushi Kittaka
, Masaaki Kurihara

Faculty of Pharmaceutical Sciences

Research output: Contribution to journal › Article › peer-review

32 Scopus citations

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.

Original language	English
Pages (from-to)	120-123
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	18
Issue number	1
DOIs	https://doi.org/10.1016/j.bmcl.2007.11.007
State	Published - 1 Jan 2008

Keywords

(2S,2′R)-LG190178
Non-secosteroidal ligand
Vitamin D receptor
YR301

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1016/j.bmcl.2007.11.007

Cite this

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title = "(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.",

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author = "Wataru Hakamata and Yukiko Sato and Haruhiro Okuda and Shinobu Honzawa and Nozomi Saito and Seishi Kishimoto and Atsushi Yamashita and Takayuki Sugiura and Atsushi Kittaka and Masaaki Kurihara",

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T1 - (2S,2′R)-Analogue of LG190178 is a major active isomer

AU - Hakamata, Wataru

AU - Sato, Yukiko

AU - Okuda, Haruhiro

AU - Honzawa, Shinobu

AU - Saito, Nozomi

AU - Kishimoto, Seishi

AU - Yamashita, Atsushi

AU - Sugiura, Takayuki

AU - Kittaka, Atsushi

AU - Kurihara, Masaaki

PY - 2008/1/1

Y1 - 2008/1/1

N2 - 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.

AB - 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.

KW - (2S,2′R)-LG190178

KW - Non-secosteroidal ligand

KW - Vitamin D receptor

KW - YR301

UR - https://www.scopus.com/pages/publications/37549005177

U2 - 10.1016/j.bmcl.2007.11.007

DO - 10.1016/j.bmcl.2007.11.007

M3 - 記事

C2 - 18054230

AN - SCOPUS:37549005177

SN - 0960-894X

VL - 18

SP - 120

EP - 123

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 1

ER -

(2S,2′R)-Analogue of LG190178 is a major active isomer

Abstract

Keywords

UN SDGs

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