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Design, Synthesis, and Biological Activity of 1,2,3-Triazolobenzodiazepine BET Bromodomain Inhibitors.

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Title: Design, Synthesis, and Biological Activity of 1,2,3-Triazolobenzodiazepine BET Bromodomain Inhibitors.
Authors: Sharp PP; Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, VIC 3052, Australia.; Department of Medical Biology, The University of Melbourne, Melbourne, VIC 3010, Australia., Garnier JM; Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, VIC 3052, Australia.; Department of Medical Biology, The University of Melbourne, Melbourne, VIC 3010, Australia., Hatfaludi T; Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, VIC 3052, Australia.; Department of Medical Biology, The University of Melbourne, Melbourne, VIC 3010, Australia., Xu Z; Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, VIC 3052, Australia.; Department of Medical Biology, The University of Melbourne, Melbourne, VIC 3010, Australia., Segal D; Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, VIC 3052, Australia.; Department of Medical Biology, The University of Melbourne, Melbourne, VIC 3010, Australia., Jarman KE; Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, VIC 3052, Australia.; Department of Medical Biology, The University of Melbourne, Melbourne, VIC 3010, Australia., Jousset H; Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, VIC 3052, Australia.; Department of Medical Biology, The University of Melbourne, Melbourne, VIC 3010, Australia., Garnham A; Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, VIC 3052, Australia.; Department of Medical Biology, The University of Melbourne, Melbourne, VIC 3010, Australia., Feutrill JT; Synthesis MedChem, 399 Royal Parade, Parkville, VIC 3052, Australia., Cuzzupe A; Synthesis MedChem, 399 Royal Parade, Parkville, VIC 3052, Australia., Hall P; Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, VIC 3052, Australia.; Department of Medical Biology, The University of Melbourne, Melbourne, VIC 3010, Australia., Taylor S; St. Vincent's Institute of Medical Research and Department of Medicine, St Vincent's Hospital, University of Melbourne, Fitzroy, VIC 3052, Australia., Walkley CR; St. Vincent's Institute of Medical Research and Department of Medicine, St Vincent's Hospital, University of Melbourne, Fitzroy, VIC 3052, Australia., Tyler D; Cancer Research Division, Peter MacCallum Cancer Centre, Melbourne, VIC 3000, Australia., Dawson MA; Cancer Research Division, Peter MacCallum Cancer Centre, Melbourne, VIC 3000, Australia.; Department of Haematology, Peter MacCallum Cancer Centre, Melbourne, VIC 3000, Australia.; Sir Peter MacCallum Department of Oncology, The University of Melbourne, East Melbourne, VIC 3002, Australia., Czabotar P; Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, VIC 3052, Australia.; Department of Medical Biology, The University of Melbourne, Melbourne, VIC 3010, Australia., Wilks AF; Synthesis MedChem, 399 Royal Parade, Parkville, VIC 3052, Australia., Glaser S; Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, VIC 3052, Australia.; Department of Medical Biology, The University of Melbourne, Melbourne, VIC 3010, Australia., Huang DCS; Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, VIC 3052, Australia.; Department of Medical Biology, The University of Melbourne, Melbourne, VIC 3010, Australia., Burns CJ; Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, VIC 3052, Australia.; Department of Medical Biology, The University of Melbourne, Melbourne, VIC 3010, Australia.; School of Chemistry, The Bio21 Institute, The University of Melbourne, Melbourne, VIC 3010, Australia.
Source: ACS medicinal chemistry letters [ACS Med Chem Lett] 2017 Nov 14; Vol. 8 (12), pp. 1298-1303. Date of Electronic Publication: 2017 Nov 14 (Print Publication: 2017).
Publication Type: Journal Article
Journal Info: Publisher: American Chemical Society Country of Publication: United States NLM ID: 101521073 Publication Model: eCollection Cited Medium: Print ISSN: 1948-5875 (Print) Linking ISSN: 19485875 NLM ISO Abbreviation: ACS Med Chem Lett Subsets: PubMed not MEDLINE
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  Data: Design, Synthesis, and Biological Activity of 1,2,3-Triazolobenzodiazepine BET Bromodomain Inhibitors.
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  Data: <searchLink fieldCode="AU" term="%22Sharp+PP%22">Sharp PP</searchLink>; Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, VIC 3052, Australia.; Department of Medical Biology, The University of Melbourne, Melbourne, VIC 3010, Australia.<br /><searchLink fieldCode="AU" term="%22Garnier+JM%22">Garnier JM</searchLink>; Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, VIC 3052, Australia.; Department of Medical Biology, The University of Melbourne, Melbourne, VIC 3010, Australia.<br /><searchLink fieldCode="AU" term="%22Hatfaludi+T%22">Hatfaludi T</searchLink>; Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, VIC 3052, Australia.; Department of Medical Biology, The University of Melbourne, Melbourne, VIC 3010, Australia.<br /><searchLink fieldCode="AU" term="%22Xu+Z%22">Xu Z</searchLink>; Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, VIC 3052, Australia.; Department of Medical Biology, The University of Melbourne, Melbourne, VIC 3010, Australia.<br /><searchLink fieldCode="AU" term="%22Segal+D%22">Segal D</searchLink>; Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, VIC 3052, Australia.; Department of Medical Biology, The University of Melbourne, Melbourne, VIC 3010, Australia.<br /><searchLink fieldCode="AU" term="%22Jarman+KE%22">Jarman KE</searchLink>; Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, VIC 3052, Australia.; Department of Medical Biology, The University of Melbourne, Melbourne, VIC 3010, Australia.<br /><searchLink fieldCode="AU" term="%22Jousset+H%22">Jousset H</searchLink>; Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, VIC 3052, Australia.; Department of Medical Biology, The University of Melbourne, Melbourne, VIC 3010, Australia.<br /><searchLink fieldCode="AU" term="%22Garnham+A%22">Garnham A</searchLink>; Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, VIC 3052, Australia.; Department of Medical Biology, The University of Melbourne, Melbourne, VIC 3010, Australia.<br /><searchLink fieldCode="AU" term="%22Feutrill+JT%22">Feutrill JT</searchLink>; Synthesis MedChem, 399 Royal Parade, Parkville, VIC 3052, Australia.<br /><searchLink fieldCode="AU" term="%22Cuzzupe+A%22">Cuzzupe A</searchLink>; Synthesis MedChem, 399 Royal Parade, Parkville, VIC 3052, Australia.<br /><searchLink fieldCode="AU" term="%22Hall+P%22">Hall P</searchLink>; Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, VIC 3052, Australia.; Department of Medical Biology, The University of Melbourne, Melbourne, VIC 3010, Australia.<br /><searchLink fieldCode="AU" term="%22Taylor+S%22">Taylor S</searchLink>; St. Vincent's Institute of Medical Research and Department of Medicine, St Vincent's Hospital, University of Melbourne, Fitzroy, VIC 3052, Australia.<br /><searchLink fieldCode="AU" term="%22Walkley+CR%22">Walkley CR</searchLink>; St. Vincent's Institute of Medical Research and Department of Medicine, St Vincent's Hospital, University of Melbourne, Fitzroy, VIC 3052, Australia.<br /><searchLink fieldCode="AU" term="%22Tyler+D%22">Tyler D</searchLink>; Cancer Research Division, Peter MacCallum Cancer Centre, Melbourne, VIC 3000, Australia.<br /><searchLink fieldCode="AU" term="%22Dawson+MA%22">Dawson MA</searchLink>; Cancer Research Division, Peter MacCallum Cancer Centre, Melbourne, VIC 3000, Australia.; Department of Haematology, Peter MacCallum Cancer Centre, Melbourne, VIC 3000, Australia.; Sir Peter MacCallum Department of Oncology, The University of Melbourne, East Melbourne, VIC 3002, Australia.<br /><searchLink fieldCode="AU" term="%22Czabotar+P%22">Czabotar P</searchLink>; Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, VIC 3052, Australia.; Department of Medical Biology, The University of Melbourne, Melbourne, VIC 3010, Australia.<br /><searchLink fieldCode="AU" term="%22Wilks+AF%22">Wilks AF</searchLink>; Synthesis MedChem, 399 Royal Parade, Parkville, VIC 3052, Australia.<br /><searchLink fieldCode="AU" term="%22Glaser+S%22">Glaser S</searchLink>; Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, VIC 3052, Australia.; Department of Medical Biology, The University of Melbourne, Melbourne, VIC 3010, Australia.<br /><searchLink fieldCode="AU" term="%22Huang+DCS%22">Huang DCS</searchLink>; Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, VIC 3052, Australia.; Department of Medical Biology, The University of Melbourne, Melbourne, VIC 3010, Australia.<br /><searchLink fieldCode="AU" term="%22Burns+CJ%22">Burns CJ</searchLink>; Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, VIC 3052, Australia.; Department of Medical Biology, The University of Melbourne, Melbourne, VIC 3010, Australia.; School of Chemistry, The Bio21 Institute, The University of Melbourne, Melbourne, VIC 3010, Australia.
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