Article ID Journal Published Year Pages File Type
7795865 European Journal of Medicinal Chemistry 2018 40 Pages PDF
Abstract
97Comp.EC50 (μM)IC50 (μM)Improved potency (Hit-01 to 7b)PI3Kα H1047R mutantPI3Kα WTHCT116Hit-0176.0NT>10076.0/0.137 > 500 (enzymatic level)7b0.1370.09311.2100/11.2 > 9 (cellular level)
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Related Topics
Physical Sciences and Engineering Chemistry Organic Chemistry
Preview
Difuran-substituted quinoxalines as a novel class of PI3Kα H1047R mutant inhibitors: Synthesis, biological evaluation and structure-activity relationship
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