Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 2. Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives

Journal of Medicinal Chemistry

Volumn 59, Issue 4, 2016, Pages 1370-1387

  Westaway, Susan M ^a   Preston, Alex G S ^a   Barker, Michael D ^a   Brown, Fiona ^a   Brown, Jack A ^a   Campbell, Matthew ^a   Chung, Chun Wa ^a   Drewes, Gerard ^a   Eagle, Robert ^a   Garton, Neil ^a   Gordon, Laurie ^a   Haslam, Carl ^a   Hayhow, Thomas G ^a   Humphreys, Philip G ^a   Joberty, Gerard ^a   Katso, Roy ^a   Kruidenier, Laurens ^a,c   Leveridge, Melanie ^a   Pemberton, Michelle ^a   Rioja, Inma ^a   Seal, Gail A ^a   Shipley, Tracy ^a   Singh, Onkar ^a   Suckling, Colin J ^b   Taylor, Joanna ^a   Thomas, Pamela ^a   Wilson, David M ^a,d   Lee, Kevin ^a,e   Prinjha, Rab K ^a   more..

^a GLAXOSMITHKLINE   (United Kingdom)

^b UNIVERSITY OF STRATHCLYDE   (United Kingdom)

^c ASTRAZENECA   (United Kingdom)

^d Babraham Research Campus   (United Kingdom)

^e TAKEDA PHARMACEUTICALS   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 [(1 BENZYL 1H PYRAZOL 4 YL)OXY]PYRIDO[3,4 D]PYRIMIDIN 4(3H) ONE; HISTONE DEMETHYLASE; HISTONE LYSINE DEMETHYLASE INHIBITOR; KDM4 ENZYME; KDM5 ENZYME; OXYGENASE INHIBITOR; PYRIDO[3,4 D]PYRIMIDIN 4(3H) ONE DERIVATIVE; PYRIMIDINONE DERIVATIVE; UNCLASSIFIED DRUG; ENZYME INHIBITOR; KDM4C PROTEIN, HUMAN; KDM4D PROTEIN, HUMAN; KDM5C PROTEIN, HUMAN;

ARTICLE; CELL ACTIVITY; DRUG ACTIVITY; DRUG IDENTIFICATION; DRUG STRUCTURE; LIPOPHILICITY; ANTAGONISTS AND INHIBITORS; CELL LINE; CELL MEMBRANE PERMEABILITY; CHEMICAL STRUCTURE; CHEMISTRY; HUMAN; METABOLISM; MOLECULAR DOCKING; STRUCTURE ACTIVITY RELATION; X RAY CRYSTALLOGRAPHY;

CELL LINE; CELL MEMBRANE PERMEABILITY; CRYSTALLOGRAPHY, X-RAY; ENZYME INHIBITORS; HISTONE DEMETHYLASES; HUMANS; JUMONJI DOMAIN-CONTAINING HISTONE DEMETHYLASES; MODELS, MOLECULAR; MOLECULAR DOCKING SIMULATION; PYRIMIDINONES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84959418926     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/acs.jmedchem.5b01538     Document Type: Article

References (14)

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12. This work was originally disclosed as part of an oral presentation: Westaway, S. M. Novel cell active inhibitors of histone lysine demethylases (KDMs): Progress and challenges in the discovery of tool inhibitors of JumonjiD2 (JmjD2) and JumonjiD3 (JmjD3). Abstracts of Papers, 246th National Meeting and Exposition of the American Chemical Society, Indianapolis, IN, U.S., September 8-12, 2013; American Chemical Society: Washington, DC, 2013; MEDI-26.
13. Compounds 21, 24, 25, 29, 35, 36, and 41 have also been disclosed as KDM inhibitors in the following patent application: Kanouni, T.; Stafford, J. A.; Veal, J. M.; Wallace, M. B. Histone demethylase inhibitors. PCT Int. Appl. WO2014151106, 2014.
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