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Discovery and Optimization of 2H-1λ2-Pyridin-2-one Inhibitors of Mutant Isocitrate Dehydrogenase 1 for the Treatment of Cancer.

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Title: Discovery and Optimization of 2H-1λ2-Pyridin-2-one Inhibitors of Mutant Isocitrate Dehydrogenase 1 for the Treatment of Cancer.
Authors: Rohde JM; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States., Karavadhi S; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States., Pragani R; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States., Liu L; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States., Fang Y; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States., Zhang W; Center for Integrative Chemical Biology and Drug Discovery, Division for Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27514, United States., McIver A; Center for Integrative Chemical Biology and Drug Discovery, Division for Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27514, United States., Zheng H; Center for Integrative Chemical Biology and Drug Discovery, Division for Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27514, United States., Liu Q; Center for Integrative Chemical Biology and Drug Discovery, Division for Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27514, United States., Davis MI; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States., Urban DJ; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States., Lee TD; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States., Cheff DM; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States., Hollingshead M; Biological Testing Branch, Developmental Therapeutics Program, National Cancer Institute, Frederick, Maryland 21702, United States., Henderson MJ; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States., Martinez NJ; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States., Brimacombe KR; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States., Yasgar A; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States., Zhao W; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States., Klumpp-Thomas C; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States., Michael S; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States., Covey J; Developmental Therapeutics Program Division of Cancer Treatment and Diagnosis, National Cancer Institute, Rockville, Maryland 20850, United States., Moore WJ; NExT Program Support, Applied/Developmental Research Directorate, Leidos Biomedical Research, Inc., Frederick National Laboratory for Cancer Research, Frederick, Maryland 21702, United States., Stott GM; NExT Program Support, Applied/Developmental Research Directorate, Leidos Biomedical Research, Inc., Frederick National Laboratory for Cancer Research, Frederick, Maryland 21702, United States., Li Z; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States., Simeonov A; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States., Jadhav A; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States., Frye S; Center for Integrative Chemical Biology and Drug Discovery, Division for Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27514, United States., Hall MD; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States., Shen M; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States., Wang X; Center for Integrative Chemical Biology and Drug Discovery, Division for Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27514, United States., Patnaik S; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States., Boxer MB; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.
Source: Journal of medicinal chemistry [J Med Chem] 2021 Apr 22; Vol. 64 (8), pp. 4913-4946. Date of Electronic Publication: 2021 Apr 06.
Publication Type: Journal Article; Research Support, N.I.H., Extramural; Research Support, N.I.H., Intramural
Journal Info: Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-4804 (Electronic) Linking ISSN: 00222623 NLM ISO Abbreviation: J Med Chem Subsets: MEDLINE
Database: MEDLINE Ultimate
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PubType: Academic Journal
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  Data: Discovery and Optimization of 2H-1λ<superscript>2</superscript>-Pyridin-2-one Inhibitors of Mutant Isocitrate Dehydrogenase 1 for the Treatment of Cancer.
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  Data: <searchLink fieldCode="AU" term="%22Rohde+JM%22">Rohde JM</searchLink>; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.<br /><searchLink fieldCode="AU" term="%22Karavadhi+S%22">Karavadhi S</searchLink>; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.<br /><searchLink fieldCode="AU" term="%22Pragani+R%22">Pragani R</searchLink>; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.<br /><searchLink fieldCode="AU" term="%22Liu+L%22">Liu L</searchLink>; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.<br /><searchLink fieldCode="AU" term="%22Fang+Y%22">Fang Y</searchLink>; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.<br /><searchLink fieldCode="AU" term="%22Zhang+W%22">Zhang W</searchLink>; Center for Integrative Chemical Biology and Drug Discovery, Division for Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27514, United States.<br /><searchLink fieldCode="AU" term="%22McIver+A%22">McIver A</searchLink>; Center for Integrative Chemical Biology and Drug Discovery, Division for Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27514, United States.<br /><searchLink fieldCode="AU" term="%22Zheng+H%22">Zheng H</searchLink>; Center for Integrative Chemical Biology and Drug Discovery, Division for Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27514, United States.<br /><searchLink fieldCode="AU" term="%22Liu+Q%22">Liu Q</searchLink>; Center for Integrative Chemical Biology and Drug Discovery, Division for Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27514, United States.<br /><searchLink fieldCode="AU" term="%22Davis+MI%22">Davis MI</searchLink>; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.<br /><searchLink fieldCode="AU" term="%22Urban+DJ%22">Urban DJ</searchLink>; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.<br /><searchLink fieldCode="AU" term="%22Lee+TD%22">Lee TD</searchLink>; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.<br /><searchLink fieldCode="AU" term="%22Cheff+DM%22">Cheff DM</searchLink>; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.<br /><searchLink fieldCode="AU" term="%22Hollingshead+M%22">Hollingshead M</searchLink>; Biological Testing Branch, Developmental Therapeutics Program, National Cancer Institute, Frederick, Maryland 21702, United States.<br /><searchLink fieldCode="AU" term="%22Henderson+MJ%22">Henderson MJ</searchLink>; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.<br /><searchLink fieldCode="AU" term="%22Martinez+NJ%22">Martinez NJ</searchLink>; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.<br /><searchLink fieldCode="AU" term="%22Brimacombe+KR%22">Brimacombe KR</searchLink>; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.<br /><searchLink fieldCode="AU" term="%22Yasgar+A%22">Yasgar A</searchLink>; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.<br /><searchLink fieldCode="AU" term="%22Zhao+W%22">Zhao W</searchLink>; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.<br /><searchLink fieldCode="AU" term="%22Klumpp-Thomas+C%22">Klumpp-Thomas C</searchLink>; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.<br /><searchLink fieldCode="AU" term="%22Michael+S%22">Michael S</searchLink>; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.<br /><searchLink fieldCode="AU" term="%22Covey+J%22">Covey J</searchLink>; Developmental Therapeutics Program Division of Cancer Treatment and Diagnosis, National Cancer Institute, Rockville, Maryland 20850, United States.<br /><searchLink fieldCode="AU" term="%22Moore+WJ%22">Moore WJ</searchLink>; NExT Program Support, Applied/Developmental Research Directorate, Leidos Biomedical Research, Inc., Frederick National Laboratory for Cancer Research, Frederick, Maryland 21702, United States.<br /><searchLink fieldCode="AU" term="%22Stott+GM%22">Stott GM</searchLink>; NExT Program Support, Applied/Developmental Research Directorate, Leidos Biomedical Research, Inc., Frederick National Laboratory for Cancer Research, Frederick, Maryland 21702, United States.<br /><searchLink fieldCode="AU" term="%22Li+Z%22">Li Z</searchLink>; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.<br /><searchLink fieldCode="AU" term="%22Simeonov+A%22">Simeonov A</searchLink>; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.<br /><searchLink fieldCode="AU" term="%22Jadhav+A%22">Jadhav A</searchLink>; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.<br /><searchLink fieldCode="AU" term="%22Frye+S%22">Frye S</searchLink>; Center for Integrative Chemical Biology and Drug Discovery, Division for Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27514, United States.<br /><searchLink fieldCode="AU" term="%22Hall+MD%22">Hall MD</searchLink>; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.<br /><searchLink fieldCode="AU" term="%22Shen+M%22">Shen M</searchLink>; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.<br /><searchLink fieldCode="AU" term="%22Wang+X%22">Wang X</searchLink>; Center for Integrative Chemical Biology and Drug Discovery, Division for Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27514, United States.<br /><searchLink fieldCode="AU" term="%22Patnaik+S%22">Patnaik S</searchLink>; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.<br /><searchLink fieldCode="AU" term="%22Boxer+MB%22">Boxer MB</searchLink>; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.
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  Data: <searchLink fieldCode="JN" term="%229716531%22">Journal of medicinal chemistry</searchLink> [J Med Chem] 2021 Apr 22; Vol. 64 (8), pp. 4913-4946. <i>Date of Electronic Publication: </i>2021 Apr 06.
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