Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3

Journal of Medicinal Chemistry

Volumn 56, Issue 20, 2013, Pages 8032-8048

  Goodfellow, Val S ^a   Loweth, Colin J ^a,d   Ravula, Satheesh B ^a,e   Wiemann, Torsten ^a   Nguyen, Thong ^a   Xu, Yang ^c,f   Todd, Daniel E ^c   Sheppard, David ^c   Pollack, Scott ^c   Polesskaya, Oksana ^b   Marker, Daniel F ^b   Dewhurst, Stephen ^b   Gelbard, Harris A ^b  

^a Califia Bio   (United States)

^b UNIVERSITY OF ROCHESTER SCHOOL OF MEDICINE AND DENTISTRY   (United States)

^c BioFocus DPI   (United Kingdom)

^d DART NEUROSCIENCE LLC   (United States)

^e Epigen Biosciences Inc   (United States)

^f Ropes and Gray LLP   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CEP 1347; CYTOKINE; LEUCINE RICH REPEAT KINASE 2; MIXED LINEAGE KINASE 3; PROTEIN SERINE THREONINE KINASE INHIBITOR; STRESS ACTIVATED PROTEIN KINASE; TRANSACTIVATOR PROTEIN; TUMOR NECROSIS FACTOR ALPHA; UNCLASSIFIED DRUG; URMC 099;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; BINDING AFFINITY; BLOOD BRAIN BARRIER; CONTROLLED STUDY; DRUG BINDING SITE; DRUG BIOAVAILABILITY; DRUG SYNTHESIS; ENZYME SPECIFICITY; HUMAN; HUMAN CELL; HUMAN IMMUNODEFICIENCY VIRUS 1; IC 50; MICROGLIA; MOLECULAR MODEL; MONOCYTE; MOUSE; NONHUMAN; UPREGULATION;

ADMINISTRATION, ORAL; ANIMALS; AREA UNDER CURVE; BIOLOGICAL AVAILABILITY; BLOOD-BRAIN BARRIER; BRAIN; CARBAZOLES; CELLS, CULTURED; COGNITION DISORDERS; DRUG DISCOVERY; HIV INFECTIONS; HUMANS; JNK MITOGEN-ACTIVATED PROTEIN KINASES; MALE; MAP KINASE KINASE KINASES; MICE; MICE, INBRED C57BL; MODELS, CHEMICAL; MOLECULAR STRUCTURE; MONOCYTES; PHOSPHORYLATION; PROTEIN KINASE INHIBITORS; PYRIDINES; PYRROLES; TAT GENE PRODUCTS, HUMAN IMMUNODEFICIENCY VIRUS; TUMOR NECROSIS FACTOR-ALPHA;

EID: 84886452695     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm401094t     Document Type: Article

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