Structure-based design of substituted hexafluoroisopropanol- arylsulfonamides as modulators of RORc

Bioorganic and Medicinal Chemistry Letters

Volumn 23, Issue 24, 2013, Pages 6604-6609

  Fauber, Benjamin P ^a   De Leon Boenig, Gladys ^a   Burton, Brenda ^b   Eidenschenk, Céline ^a   Everett, Christine ^a   Gobbi, Alberto ^a   Hymowitz, Sarah G ^a   Johnson, Adam R ^a   Liimatta, Marya ^a   Lockey, Peter ^b   Norman, Maxine ^b   Ouyang, Wenjun ^a   René, Olivier ^a   Wong, Harvey ^a  

^a GENENTECH INC   (United States)

^b Argenta Discovery Ltd   (United Kingdom)

Author keywords

Autoimmune; IL 17; Inflammation; ROR ; RORc; T0901317; X ray structure

Indexed keywords

INTERLEUKIN 17; N (2,2,2 TRIFLUOROETHYL) N [4 (2,2,2 TRIFLUORO 1 HYDROXY 1 TRIFLUOROMETHYLETHYL)PHENYL]BENZENESULFONAMIDE; RETINOID RELATED ORPHAN RECEPTOR GAMMA; SULFONAMIDE;

ARTICLE; BINDING AFFINITY; CONTROLLED STUDY; CRYSTAL STRUCTURE; CYTOKINE PRODUCTION; DRUG DESIGN; DRUG SYNTHESIS; HUMAN; HUMAN CELL; HYDROGEN BOND; LIGAND BINDING; LIPOPHILICITY; PROTEIN EXPRESSION; STRUCTURE ACTIVITY RELATION; X RAY CRYSTALLOGRAPHY;

AUTOIMMUNE; IL-17; INFLAMMATION; RORC; RORΓ; T0901317; X-RAY STRUCTURE;

BINDING SITES; CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; DRUG INVERSE AGONISM; HUMANS; HYDROCARBONS, FLUORINATED; INTERFERON-GAMMA; INTERLEUKIN-17; LEUKOCYTES, MONONUCLEAR; MOLECULAR DYNAMICS SIMULATION; NUCLEAR RECEPTOR SUBFAMILY 1, GROUP F, MEMBER 3; PROPANOLS; PROTEIN BINDING; PROTEIN STRUCTURE, TERTIARY; STRUCTURE-ACTIVITY RELATIONSHIP; SULFONAMIDES;

EID: 84888857603     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2013.10.054     Document Type: Article

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