Extending SAR of bile acids as FXR ligands: Discovery of 23-N-(carbocinnamyloxy)-3α,7α-dihydroxy-6α-ethyl-24-nor- 5β-cholan-23-amine

Bioorganic and Medicinal Chemistry

Volumn 19, Issue 8, 2011, Pages 2650-2658

  Gioiello, Antimo ^a   MacChiarulo, Antonio ^a   Carotti, Andrea ^a   Filipponi, Paolo ^a   Costantino, Gabriele ^b   Rizzo, Giovanni ^c   Adorini, Luciano ^c   Pellicciari, Roberto ^a  

^a UNIVERSITY OF PERUGIA   (Italy)

^b UNIVERSITY OF PARMA   (Italy)

^c INTERCEPT PHARMACEUTICALS   (United States)

Author keywords

Allosteric site; Bile acid; Carbamate; FXR; RMDS

Indexed keywords

23 N (CARBOCINNAMYLOXY) 3ALPHA,7ALPHA DIHYDROXY 6ALPHA ETHYL 24 NOR 5BETA CHOLAN 23 AMINE; 3ALPHA, 7ALPHA DIFORMYLOXY 6ALPHA ETHYL 5BETA CHOLAN 24 OIC ACID; 3ALPHA, 7ALPHA DIHYDROXY 6ALPHA ETHYL 5BETA CHOLAN 24 OIC ACID; BILE ACID; FARNESOID X RECEPTOR STIMULATING AGENT; HORMONE RECEPTOR STIMULATING AGENT; MESSENGER RNA; UNCLASSIFIED DRUG;

ARTICLE; BINDING AFFINITY; CELL STRAIN HEK293; CELL STRAIN HEPG2; CHEMICAL MODIFICATION; CONTROLLED STUDY; DRUG EFFICACY; DRUG MECHANISM; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SCREENING; DRUG STRUCTURE; DRUG SYNTHESIS; HUMAN; HUMAN CELL; MOLECULAR DOCKING; MOLECULAR DYNAMICS; RECEPTOR UPREGULATION; REVERSE TRANSCRIPTION POLYMERASE CHAIN REACTION; STRUCTURE ACTIVITY RELATION;

BILE ACIDS AND SALTS; COMPUTER SIMULATION; DRUG DISCOVERY; GASTROINTESTINAL AGENTS; LIGANDS; PROTEIN BINDING; RECEPTORS, CYTOPLASMIC AND NUCLEAR; REVERSE TRANSCRIPTASE POLYMERASE CHAIN REACTION; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 79954416610     PISSN: 09680896     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmc.2011.03.004     Document Type: Article

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