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

Author:

Rohde Jason M.1,Karavadhi Surendra1,Pragani Rajan1,Liu Li1,Fang Yuhong1,Zhang Weihe2,McIver Andrew2,Zheng Hongchao2,Liu Qingyang2,Davis Mindy I.1,Urban Daniel J.1,Lee Tobie D.1,Cheff Dorian M.1,Hollingshead Melinda3,Henderson Mark J.1ORCID,Martinez Natalia J.1,Brimacombe Kyle R.1,Yasgar Adam1ORCID,Zhao Wei1ORCID,Klumpp-Thomas Carleen1,Michael Sam1,Covey Joseph4,Moore William J.5,Stott Gordon M.5,Li Zhuyin1,Simeonov Anton1,Jadhav Ajit1,Frye Stephen2ORCID,Hall Matthew D.1ORCID,Shen Min1,Wang Xiaodong2ORCID,Patnaik Samarjit1ORCID,Boxer Matthew B.1

Affiliation:

1. National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States

2. 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

3. Biological Testing Branch, Developmental Therapeutics Program, National Cancer Institute, Frederick, Maryland 21702, United States

4. Developmental Therapeutics Program Division of Cancer Treatment and Diagnosis, National Cancer Institute, Rockville, Maryland 20850, United States

5. NExT Program Support, Applied/Developmental Research Directorate, Leidos Biomedical Research, Inc., Frederick National Laboratory for Cancer Research, Frederick, Maryland 21702, United States

Funder

National Center for Advancing Translational Sciences

National Cancer Institute

National Institute of Mental Health

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

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