Structural development of liver X receptor (LXR) antagonists derived from thalidomide-related glucosidase inhibitors.
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.
Noguchi-Yachide
Tomomi
T
Institute of Molecular & Cellular Biosciences, The University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-0032, Japan.
Miyachi
Hiroyuki
H
Aoyama
Hiroshi
H
Aoyama
Atsushi
A
Makishima
Makoto
M
Hashimoto
Yuichi
Y
D045744:Cell Line, Tumor; D004268:DNA-Binding Proteins / Q000037:antagonists & inhibitors*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D017930:Genes, Reporter / Q000235:genetics; D005959:Glucosidases / Q000037:antagonists & inhibitors*; D006801:Humans; D006993:Hypnotics and Sedatives / Q000737:chemistry / Q000494:pharmacology*; D007202:Indicators and Reagents; D000071518:Liver X Receptors; D009682:Magnetic Resonance Spectroscopy; D057093:Orphan Nuclear Receptors; D010797:Phthalimides / Q000138:chemical synthesis* / Q000494:pharmacology*; D018160:Receptors, Cytoplasmic and Nuclear / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D013792:Thalidomide / Q000737:chemistry / Q000494:pharmacology*
C526058:5-chloro-N-2'-n-pentylphenyl-1,3-dithiophthalimide; D004268:DNA-Binding Proteins; D004791:Enzyme Inhibitors; D006993:Hypnotics and Sedatives; D007202:Indicators and Reagents; D000071518:Liver X Receptors; C000605213:NR1H3 protein, human; D057093:Orphan Nuclear Receptors; D010797:Phthalimides; D018160:Receptors, Cytoplasmic and Nuclear; D013792:Thalidomide; D005959:Glucosidases