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Discovery and Optimization of 2H-1λ2-Pyridin-2-one Inhibitors of Mutant Isocitrate Dehydrogenase 1 for the Treatment of Cancer.
Rohde, Jason M; Karavadhi, Surendra; Pragani, Rajan; Liu, Li; Fang, Yuhong; Zhang, Weihe; McIver, Andrew; Zheng, Hongchao; Liu, Qingyang; Davis, Mindy I; Urban, Daniel J; Lee, Tobie D; Cheff, Dorian M; Hollingshead, Melinda; Henderson, Mark J; Martinez, Natalia J; Brimacombe, Kyle R; Yasgar, Adam; Zhao, Wei; Klumpp-Thomas, Carleen; Michael, Sam; Covey, Joseph; Moore, William J; Stott, Gordon M; Li, Zhuyin; Simeonov, Anton; Jadhav, Ajit; Frye, Stephen; Hall, Matthew D; Shen, Min; Wang, Xiaodong; Patnaik, Samarjit; Boxer, Matthew B.
Affiliation
  • 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.
J Med Chem ; 64(8): 4913-4946, 2021 04 22.
Article in En | MEDLINE | ID: mdl-33822623
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Pyridones / Enzyme Inhibitors / Isocitrate Dehydrogenase Limits: Animals / Female / Humans Language: En Journal: J Med Chem Journal subject: QUIMICA Year: 2021 Type: Article Affiliation country: United States
Fulltext
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PubMed Links
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Pyridones / Enzyme Inhibitors / Isocitrate Dehydrogenase Limits: Animals / Female / Humans Language: En Journal: J Med Chem Journal subject: QUIMICA Year: 2021 Type: Article Affiliation country: United States