Discovery and Optimization of 2<i>H</i>-1λ<sup>2</sup>-Pyridin-2-one Inhibitors of Mutant Isocitrate Dehydrogenase 1 for the Treatment of Cancer
Jason M. Rohde, Karavadhi Surendra, Rajan Pragani, Li Liu, Yuhong Fang, Weihe Zhang, Andrew L. McIver, Hongchao Zheng, Qingyang Liu, Mindy I. Davis, Daniel J. Urban, Tobie D. Lee, Dorian M. Cheff, Melinda G. Hollingshead, Mark J. Henderson, Natalia J. Martinez, Kyle R. Brimacombe, Adam Yasgar, Wei Zhao, Carleen Klumpp‐Thomas, Sam Michael, Joseph M. Covey, William Moore, Gordon M. Stott, Zhuyin Li, Anton Simeonov, Ajit Jadhav, Stephen V. Frye, Matthew D. Hall, Min Shen, Xiaodong Wang, Samarjit Patnaik, Matthew B. Boxer
Abstract
showed higher tumoral concentrations that corresponded to lower 2-HG concentrations, when compared with the approved drug AG-120 (ivosidenib).
Topics & Concepts
ChemistryIsocitrate dehydrogenaseMutantEnzymeCancerBiochemistryStereochemistryGeneGeneticsBiologyCancer, Hypoxia, and MetabolismGlioma Diagnosis and TreatmentMedical Imaging Techniques and Applications