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

T Noguchi-Yachide, H Miyachi, H Aoyama… - Chemical and …, 2007 - jstage.jst.go.jp
T Noguchi-Yachide, H Miyachi, H Aoyama, A Aoyama, M Makishima, Y Hashimoto
Chemical and Pharmaceutical Bulletin, 2007jstage.jst.go.jp
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 mM for LXRa and
LXRb, respectively.
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 mM for LXRa and LXRb, respectively.
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