Structural development of liver X receptor (LXR) antagonists derived from thalidomide-related glucosidase inhibitors

Tomomi Noguchi-Yachide; Hiroyuki Miyachi; Hiroshi Aoyama; Atsushi Aoyama; Makoto Makishima; Yuichi Hashimoto

doi:10.1248/cpb.55.1750

Structural development of liver X receptor (LXR) antagonists derived from thalidomide-related glucosidase inhibitors

Tomomi Noguchi-Yachide, Hiroyuki Miyachi, Hiroshi Aoyama, Atsushi Aoyama, Makoto Makishima, Yuichi Hashimoto

Faculty of Pharmaceutical Sciences

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

24 Citations (Scopus)

Abstract

Following our previous discovery of LXR antagonistic activity of 2′-substituted phenylphthalimides derived from thalidomide-related glucosidase inhibitors, structure-activity studies and further structural development led to 5-chloro-N-2′-n-pentylphenyl-1,3-dithiophthalimide (5CPPSS-50), with IC₅₀ values of about 10 and 13 μM for LXRα and LXR β, respectively.

Original language	English
Pages (from-to)	1750-1754
Number of pages	5
Journal	Chemical and Pharmaceutical Bulletin
Volume	55
Issue number	12
DOIs	https://doi.org/10.1248/cpb.55.1750
Publication status	Published - Dec 2007

Keywords

Antagonist
Glucosidase inhibitor
Liver X receptor
Phthalimide skeleton
Thalidomide

ASJC Scopus subject areas

Chemistry(all)
Drug Discovery

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10.1248/cpb.55.1750

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abstract = "Following our previous discovery of LXR antagonistic activity of 2′-substituted phenylphthalimides derived from thalidomide-related glucosidase inhibitors, structure-activity studies and further structural development led to 5-chloro-N-2′-n-pentylphenyl-1,3-dithiophthalimide (5CPPSS-50), with IC50 values of about 10 and 13 μM for LXRα and LXR β, respectively.",

keywords = "Antagonist, Glucosidase inhibitor, Liver X receptor, Phthalimide skeleton, Thalidomide",

author = "Tomomi Noguchi-Yachide and Hiroyuki Miyachi and Hiroshi Aoyama and Atsushi Aoyama and Makoto Makishima and Yuichi Hashimoto",

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AU - Noguchi-Yachide, Tomomi

AU - Miyachi, Hiroyuki

AU - Aoyama, Hiroshi

AU - Aoyama, Atsushi

AU - Makishima, Makoto

AU - Hashimoto, Yuichi

PY - 2007/12

Y1 - 2007/12

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AB - Following our previous discovery of LXR antagonistic activity of 2′-substituted phenylphthalimides derived from thalidomide-related glucosidase inhibitors, structure-activity studies and further structural development led to 5-chloro-N-2′-n-pentylphenyl-1,3-dithiophthalimide (5CPPSS-50), with IC50 values of about 10 and 13 μM for LXRα and LXR β, respectively.

KW - Antagonist

KW - Glucosidase inhibitor

KW - Liver X receptor

KW - Phthalimide skeleton

KW - Thalidomide

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Structural development of liver X receptor (LXR) antagonists derived from thalidomide-related glucosidase inhibitors

Abstract

Keywords

ASJC Scopus subject areas

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