Identification and structure activity relationships of quinoline tertiary alcohol modulators of RORγt

Bioorganic and Medicinal Chemistry Letters

Volumn 27, Issue 9, 2017, Pages 2047-2057

  Kummer, David A ^a   Cummings, Maxwell D ^a   Abad, Marta ^a   Barbay, Joseph ^a   Castro, Glenda ^a   Wolin, Ronald ^a   Kreutter, Kevin D ^a   Maharoof, Umar ^a   Milligan, Cynthia ^a   Nishimura, Rachel ^a   Pierce, Joan ^a   Schalk Hihi, Celine ^a   Spurlino, John ^a   Urbanski, Maud ^a   Venkatesan, Hariharan ^a   Wang, Aihua ^a   Woods, Craig ^a   Xue, Xiaohua ^a   Edwards, James P ^a   Fourie, Anne M ^a   Leonard, Kristi ^a   more..

^a JANSSEN RESEARCH AND DEVELOPMENT   (Belgium)

Author keywords

Agonist; IL 17; Inverse agonist; Neutral antagonist; Retinoic acid related orphan nuclear receptor gamma t; ROR t; Th17

Indexed keywords

ALCOHOL DERIVATIVE; KETONE DERIVATIVE; PROTEIN INHIBITOR; QUINOLINE DERIVATIVE; RETINOID RELATED ORPHAN RECEPTOR GAMMA;

AGONIST; ARTICLE; BINDING AFFINITY; CELL ASSAY; CHLORINATION; CONFORMATIONAL TRANSITION; CRYSTAL STRUCTURE; CYCLIZATION; DRUG DESIGN; DRUG IDENTIFICATION; DRUG POTENCY; DRUG SYNTHESIS; EC50; ENANTIOMER; HUMAN; IC50; LYMPHOCYTE DIFFERENTIATION; RACEMIC MIXTURE; STEREOCHEMISTRY; STRUCTURE ACTIVITY RELATION; SUPERCRITICAL FLUID CHROMATOGRAPHY; TH17 CELL; X RAY CRYSTALLOGRAPHY; ANTAGONISTS AND INHIBITORS; CHEMISTRY; DRUG EFFECTS; INVERSE AGONISM; METABOLISM; MOLECULAR DOCKING;

DRUG DESIGN; DRUG INVERSE AGONISM; HUMANS; MOLECULAR DOCKING SIMULATION; NUCLEAR RECEPTOR SUBFAMILY 1, GROUP F, MEMBER 3; QUINOLINES; STRUCTURE-ACTIVITY RELATIONSHIP; TH17 CELLS;

EID: 85015335920     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2017.02.044     Document Type: Article

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