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C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays.
Le Bihan, Yann-Vaï; Lanigan, Rachel M; Atrash, Butrus; McLaughlin, Mark G; Velupillai, Srikannathasan; Malcolm, Andrew G; England, Katherine S; Ruda, Gian Filippo; Mok, N Yi; Tumber, Anthony; Tomlin, Kathy; Saville, Harry; Shehu, Erald; McAndrew, Craig; Carmichael, LeAnne; Bennett, James M; Jeganathan, Fiona; Eve, Paul; Donovan, Adam; Hayes, Angela; Wood, Francesca; Raynaud, Florence I; Fedorov, Oleg; Brennan, Paul E; Burke, Rosemary; van Montfort, Rob L M; Rossanese, Olivia W; Blagg, Julian; Bavetsias, Vassilios.
Affiliation
  • Le Bihan YV; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, UK.
  • Lanigan RM; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, UK.
  • Atrash B; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, UK.
  • McLaughlin MG; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, UK.
  • Velupillai S; Structural Genomics Consortium (SGC), University of Oxford, ORCRB Roosevelt Drive, Oxford, OX3 7DQ, UK.
  • Malcolm AG; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, UK.
  • England KS; Structural Genomics Consortium (SGC), University of Oxford, ORCRB Roosevelt Drive, Oxford, OX3 7DQ, UK; Target Discovery Institute (TDI), Nuffield Department of Medicine, University of Oxford, NDMRB, Roosevelt Drive, Oxford, OX3 7FZ, UK.
  • Ruda GF; Structural Genomics Consortium (SGC), University of Oxford, ORCRB Roosevelt Drive, Oxford, OX3 7DQ, UK.
  • Mok NY; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, UK.
  • Tumber A; Structural Genomics Consortium (SGC), University of Oxford, ORCRB Roosevelt Drive, Oxford, OX3 7DQ, UK; Target Discovery Institute (TDI), Nuffield Department of Medicine, University of Oxford, NDMRB, Roosevelt Drive, Oxford, OX3 7FZ, UK.
  • Tomlin K; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, UK.
  • Saville H; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, UK.
  • Shehu E; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, UK.
  • McAndrew C; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, UK.
  • Carmichael L; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, UK.
  • Bennett JM; Structural Genomics Consortium (SGC), University of Oxford, ORCRB Roosevelt Drive, Oxford, OX3 7DQ, UK; Target Discovery Institute (TDI), Nuffield Department of Medicine, University of Oxford, NDMRB, Roosevelt Drive, Oxford, OX3 7FZ, UK.
  • Jeganathan F; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, UK.
  • Eve P; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, UK.
  • Donovan A; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, UK.
  • Hayes A; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, UK.
  • Wood F; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, UK.
  • Raynaud FI; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, UK.
  • Fedorov O; Structural Genomics Consortium (SGC), University of Oxford, ORCRB Roosevelt Drive, Oxford, OX3 7DQ, UK; Target Discovery Institute (TDI), Nuffield Department of Medicine, University of Oxford, NDMRB, Roosevelt Drive, Oxford, OX3 7FZ, UK.
  • Brennan PE; Structural Genomics Consortium (SGC), University of Oxford, ORCRB Roosevelt Drive, Oxford, OX3 7DQ, UK; Target Discovery Institute (TDI), Nuffield Department of Medicine, University of Oxford, NDMRB, Roosevelt Drive, Oxford, OX3 7FZ, UK.
  • Burke R; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, UK.
  • van Montfort RLM; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, UK.
  • Rossanese OW; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, UK.
  • Blagg J; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, UK. Electronic address: julian.blagg@icr.ac.uk.
  • Bavetsias V; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, UK. Electronic address: vassilios.bavetsias@icr.ac.uk.
Eur J Med Chem ; 177: 316-337, 2019 Sep 01.
Article in En | MEDLINE | ID: mdl-31158747
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Pyridines / Pyrimidinones / Enzyme Inhibitors / Jumonji Domain-Containing Histone Demethylases Type of study: Diagnostic_studies Limits: Humans Language: En Journal: Eur J Med Chem Year: 2019 Type: Article Affiliation country: United kingdom
Fulltext
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Pyridines / Pyrimidinones / Enzyme Inhibitors / Jumonji Domain-Containing Histone Demethylases Type of study: Diagnostic_studies Limits: Humans Language: En Journal: Eur J Med Chem Year: 2019 Type: Article Affiliation country: United kingdom