Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist

Journal of Medicinal Chemistry

Volumn 53, Issue 8, 2010, Pages 3296-3304

  Hu, Baihua ^a   Unwalla, Rayomand J ^c   Goljer, Igor ^a   Jetter, James W ^a   Quinet, Elaine M ^a   Berrodin, Thomas J ^a   Basso, Michael D ^a   Feingold, Irene B ^a   Nilsson, Annika Goos ^b   Wilhelmsson, Anna ^b   Evans, Mark J ^a   Wrobel, Jay E ^a  

^a PFIZER INC   (United States)

^b Karo Bio   (Sweden)

^c NONE

Author keywords

[No Author keywords available]

Indexed keywords

3 METHYL 2 [3' (METHYLSULFONYL)BIPHENYL 4 YL] 5 (TRIFLUOROMETHYL)QUINOXALINE; ABC TRANSPORTER A1; CHOLESTEROL; LIVER X RECEPTOR AGONIST; LIVER X RECEPTOR BETA; QUINOXALINE DERIVATIVE; STEROL REGULATORY ELEMENT BINDING PROTEIN 1C; SULFONE DERIVATIVE; TRANSCRIPTION FACTOR GAL4; TRIACYLGLYCEROL; UNCLASSIFIED DRUG; WYE 672;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL TISSUE; AREA UNDER THE CURVE; ARTICLE; ATHEROSCLEROSIS; BINDING AFFINITY; CHOLESTEROL BLOOD LEVEL; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG BLOOD LEVEL; DRUG HALF LIFE; DRUG POTENCY; DRUG SCREENING; DRUG SELECTIVITY; DRUG SYNTHESIS; GENE EXPRESSION; HUMAN; HUMAN CELL; KNOCKOUT MOUSE; MALE; MAXIMUM PLASMA CONCENTRATION; MOLECULAR DOCKING; MOUSE; NONHUMAN; PARTIAL AGONISM; STRUCTURE ACTIVITY RELATION; TIME TO MAXIMUM PLASMA CONCENTRATION;

ANIMALS; AREA UNDER CURVE; ATHEROSCLEROSIS; ATP-BINDING CASSETTE TRANSPORTERS; CELL LINE; CHOLESTEROL; DUODENUM; HALF-LIFE; HUMANS; KIDNEY; LIVER; MALE; MICE; MICE, INBRED C57BL; MICE, KNOCKOUT; MODELS, MOLECULAR; ORGAN SPECIFICITY; ORPHAN NUCLEAR RECEPTORS; QUINOXALINES; RADIOLIGAND ASSAY; STRUCTURE-ACTIVITY RELATIONSHIP; SULFONES; TRANSCRIPTIONAL ACTIVATION; TRIGLYCERIDES;

EID: 77951140849     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm100034x     Document Type: Article

References (31)

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