Discovery and SAR of potent, orally available 2,8-diaryl-quinoxalines as a new class of JAK2 inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 8, 2010, Pages 2609-2613

  Pissot Soldermann, Carole ^a   Gerspacher, Marc ^a   Furet, Pascal ^a   Gaul, Christoph ^a   Holzer, Philipp ^a   McCarthy, Clive ^a   Radimerski, Thomas ^a   Regnier, Catherine H ^a   Baffert, Fabienne ^a   Drueckes, Peter ^a   Tavares, Gisele A ^a   Vangrevelinghe, Eric ^a   Blasco, Francesca ^a   Ottaviani, Giorgio ^a   Ossola, Flavio ^a   Scesa, Julien ^a   Reetz, Janitha ^a  

^a NOVARTIS PHARMA AG   (Switzerland)

Author keywords

JAK1; JAK2; JAK3; Janus kinase; Kinase inhibitors; Tyk2

Indexed keywords

JANUS KINASE 2; JANUS KINASE 2 INHIBITOR; JANUS KINASE INHIBITOR; QUINOXALINE DERIVATIVE;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CELL PROLIFERATION; CONTROLLED STUDY; DRUG CLEARANCE; DRUG EFFICACY; DRUG HALF LIFE; DRUG SOLUBILITY; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME INHIBITION; GROWTH INHIBITION; HUMAN; HUMAN CELL; IN VITRO STUDY; IN VIVO STUDY; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION; THERMODYNAMICS;

ADMINISTRATION, ORAL; ANIMALS; CELL LINE; DRUG DISCOVERY; DRUG EVALUATION, PRECLINICAL; JANUS KINASE 2; MODELS, MOLECULAR; PROTEIN KINASE INHIBITORS; QUINOXALINES; RATS; STRUCTURE-ACTIVITY RELATIONSHIP;

RATTUS;

EID: 77950037732     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.02.056     Document Type: Article

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