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

T Noguchi-Yachide, H Miyachi, H Aoyama…

Index: Noguchi-Yachide, Tomomi; Miyachi, Hiroyuki; Aoyama, Hiroshi; Aoyama, Atsushi; Makishima, Makoto; Hashimoto, Yuichi Chemical and Pharmaceutical Bulletin, 2007 , vol. 55, # 12 p. 1750 - 1754

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Citation Number: 17

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 IC 50 values of about 10 and 13 μM for LXRα and LXRβ, respectively.

Synthesis of Enantiopure 1??Aryl??1??butylamines and 1??Aryl...

[Dalmolen, Jan; Van Der Sluis, Marcel; Nieuwenhuijzen, Jose W.; Meetsma, Auke; De Lange, Ben; Kaptein, Bernard; Kellogg, Richard M.; Broxterman, Quirinus B. European Journal of Organic Chemistry, 2004 , # 7 p. 1544 - 1557]