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

Notes

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

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Keywords: liver X receptor, thalidomide, phthalimide skeleton, antagonist, glucosidase inhibitor

JOURNAL FREE ACCESS

2007 Volume 55 Issue 12 Pages 1750-1754

DOI https://doi.org/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 LXRβ, respectively.

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