8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors

Journal of Medicinal Chemistry

Volumn 59, Issue 4, 2016, Pages 1388-1409

  Bavetsias, Vassilios ^a   Lanigan, Rachel M ^a   Ruda, Gian Filippo ^b,c   Atrash, Butrus ^a   McLaughlin, Mark G ^a   Tumber, Anthony ^b,c   Mok, N Yi ^a   Le Bihan, Yann Vaï ^a   Dempster, Sally ^a   Boxall, Katherine J ^a   Jeganathan, Fiona ^a   Hatch, Stephanie B ^b,c   Savitsky, Pavel ^b   Velupillai, Srikannathasan ^b   Krojer, Tobias ^b   England, Katherine S ^b,c   Sejberg, Jimmy ^a   Thai, Ching ^a   Donovan, Adam ^a   Pal, Akos ^a   Scozzafava, Giuseppe ^b,c   Bennett, James M ^b,c   Kawamura, Akane ^d   Johansson, Catrine ^b,e   Szykowska, Aleksandra ^b   Gileadi, Carina ^b   Burgess Brown, Nicola A ^b   Von Delft, Frank ^b,f,g   Oppermann, Udo ^b,e   Walters, Zoe ^a   Shipley, Janet ^a   Raynaud, Florence I ^a   Westaway, Susan M ^h   Prinjha, Rab K ^h   Fedorov, Oleg ^b,c   Burke, Rosemary ^a   Schofield, Christopher J ^d   Westwood, Isaac M ^a   Bountra, Chas ^b   Müller, Susanne ^b,c   Van Montfort, Rob L M ^a   Brennan, Paul E ^b,c   Blagg, Julian ^a   more..

^a INSTITUTE OF CANCER RESEARCH   (United Kingdom)

^b UNIVERSITY OF OXFORD   (United Kingdom)

^c UNIVERSITY OF OXFORD   (United Kingdom)

^d UNIVERSITY OF OXFORD   (United Kingdom)

^e NIHR OXFORD BIOMEDICAL RESEARCH CENTRE   (United Kingdom)

^f DIAMOND LIGHT SOURCE LTD   (United Kingdom)

^g UNIVERSITY OF JOHANNESBURG   (South Africa)

^h GLAXOSMITHKLINE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

8 (1H PYRAZOL 3 YL)PYRIDO[3,4 D]PYRIMIDIN 4(3H) ONE DERIVATIVE; HISTONE LYSINE METHYLTRANSFERASE INHIBITOR; UNCLASSIFIED DRUG; ENZYME INHIBITOR; HISTONE DEMETHYLASE; KDM4A PROTEIN, HUMAN; KDM4D PROTEIN, HUMAN; KDM5B PROTEIN, HUMAN; NUCLEAR PROTEIN; PYRIMIDINONE DERIVATIVE; REPRESSOR PROTEIN;

ARTICLE; CACO 2 CELL LINE; CELL MEMBRANE PERMEABILITY; CONFORMATIONAL TRANSITION; CONTROLLED STUDY; DRUG BINDING; DRUG DESIGN; DRUG POTENCY; DRUG SYNTHESIS; ENZYME INHIBITION; HISTONE DEMETHYLATION; HUMAN; HUMAN CELL; ANTAGONISTS AND INHIBITORS; CACO-2 CELL LINE; CHEMISTRY; METABOLISM;

CACO-2 CELLS; CELL MEMBRANE PERMEABILITY; ENZYME INHIBITORS; HUMANS; JUMONJI DOMAIN-CONTAINING HISTONE DEMETHYLASES; NUCLEAR PROTEINS; PYRIMIDINONES; REPRESSOR PROTEINS;

EID: 84959422044     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/acs.jmedchem.5b01635     Document Type: Article

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