Synthesis of novel ketoconazole derivatives as inhibitors of the human Pregnane X Receptor (PXR; NR1I2; also termed SXR, PAR)

Bioorganic and Medicinal Chemistry Letters

Volumn 18, Issue 14, 2008, Pages 3974-3977

  Das, Bhaskar C ^a   Madhukumar, Ankanahlli V ^a   Anguiano, Jaime ^a   Kim, Sean ^b   Sinz, Michael ^b   Zvyaga, Tatyana A ^b   Power, Eoin C ^c   Ganellin, C Robin ^d   Mani, Sridhar ^a  

^a ALBERT EINSTEIN COLLEGE OF MEDICINE   (United States)

^b BRISTOL MYERS SQUIBB   (United States)

^c Siena Biotech SpA   (Italy)

^d UNIVERSITY COLLEGE LONDON   (United Kingdom)

Author keywords

Analogs; Azole; Ketoconazole; Nuclear receptors; Pregnane X receptor; PXR

Indexed keywords

1 [4 [4 [2 [2 (2,4 DIFLUOROPHENYL) 2 METHYL 1,3 DIOXOLAN 4 YL]METHOXY]PHENYL]PIPERAZIN 1 YL]ETHANONE; 2',4' DIFLUOROACETOPHENONE; 4 BROMOPHENOL; ACETAL; ACETOPHENONE DERIVATIVE; BENZENE; CYTOCHROME P450; GLYCIDOL; KETOCONAZOLE; N,N DIMETHYLFORMAMIDE; PALLADIUM; PHENOL DERIVATIVE; POTASSIUM CARBONATE; PREGNANE X RECEPTOR; PYRROLE DERIVATIVE; TOLUENESULFONIC ACID; TOLUENESULFONIC ACID DERIVATIVE; UCL 2158H;

ARTICLE; CATALYSIS; CELL CULTURE; CELL LINE; CELL STRAIN CACO 2; CELL STRAIN HEPG2; CONCENTRATION RESPONSE; CULTURE MEDIUM; DRUG CYTOTOXICITY; DRUG MECHANISM; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME INHIBITION; HUMAN; HUMAN CELL; IC 50; MICROSOME; REACTION ANALYSIS; STRUCTURE ACTIVITY RELATION;

BINDING SITES; CATALYSIS; CELL LINE, TUMOR; CHEMISTRY, PHARMACEUTICAL; CYTOCHROME P-450 CYP3A; CYTOCHROME P-450 ENZYME SYSTEM; DRUG DESIGN; DRUG INTERACTIONS; HUMANS; INHIBITORY CONCENTRATION 50; KETOCONAZOLE; MICROSOMES, LIVER; MODELS, CHEMICAL; RECEPTORS, STEROID;

EID: 47149088622     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.06.018     Document Type: Article

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