Structural development of liver X receptor (LXR) antagonists derived from thalidomide-related glucosidase inhibitors |
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| Authors: | Noguchi-Yachide Tomomi Miyachi Hiroyuki Aoyama Hiroshi Aoyama Atsushi Makishima Makoto Hashimoto Yuichi |
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| Institution: | Institute of Molecular & Cellular Biosciences, The University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-0032, Japan. |
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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 microM for LXRalpha and LXRbeta, respectively. |
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