Discovery of biaryls as RORγ inverse agonists by using structure-based design

Bioorganic and Medicinal Chemistry Letters

Volumn 26, Issue 10, 2016, Pages 2459-2463

  Enyedy, Istvan J ^a   Powell, Noel A ^a   Caravella, Justin ^a   Van Vloten, Kurt ^a   Chao, Jianhua ^a   Banerjee, Daliya ^a   Marcotte, Douglas ^a   Silvian, Laura ^a   McKenzie, Andres ^a   Hong, Victor Sukbong ^b   Fontenot, Jason D ^a  

^a BIOGEN   (United States)

^b Keimyung University   (South Korea)

Author keywords

Biaryls; Retinoid related orphan receptor gamma; ROR ; Sulfonamides; Tetrahydroquinolines

Indexed keywords

ANTIINFLAMMATORY AGENT; N (2,2,2 TRIFLUOROETHYL) N [4 (2,2,2 TRIFLUORO 1 HYDROXY 1 TRIFLUOROMETHYLETHYL)PHENYL]BENZENESULFONAMIDE; RAR RELATED ORPHAN RECEPTOR GAMMA INVERSE AGONIST; UNCLASSIFIED DRUG; FLUORINATED HYDROCARBON; RETINOID RELATED ORPHAN RECEPTOR GAMMA; SULFONAMIDE; TO-901317;

ARTICLE; BINDING SITE; DRUG DESIGN; DRUG SCREENING; DRUG STRUCTURE; IC50; LIGAND BINDING; AGONISTS; CHEMICAL STRUCTURE; CHEMISTRY; METABOLISM; MOLECULAR DOCKING; MOLECULAR MODEL; STRUCTURE ACTIVITY RELATION; X RAY CRYSTALLOGRAPHY;

BINDING SITES; CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; HYDROCARBONS, FLUORINATED; MODELS, MOLECULAR; MOLECULAR DOCKING SIMULATION; MOLECULAR STRUCTURE; NUCLEAR RECEPTOR SUBFAMILY 1, GROUP F, MEMBER 3; STRUCTURE-ACTIVITY RELATIONSHIP; SULFONAMIDES;

EID: 84978328056     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2016.03.109     Document Type: Article

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