Discovery of the first known small-molecule inhibitors of heme-regulated eukaryotic initiation factor 2α (HRI) kinase
作者： Mark D. Rosen , Craig R. Woods , Steven D. Goldberg , Michael D. Hack , A. Dawn Bounds
DOI: 10.1016/J.BMCL.2009.10.033
关键词: Kinase 、 Heme 、 Structure–activity relationship 、 Biochemistry 、 Drug discovery 、 Chemistry 、 EIF-2 kinase 、 Small molecule 、 Enzyme 、 Eukaryotic initiation factor 、 Organic chemistry 、 Clinical biochemistry 、 Molecular medicine 、 Molecular biology 、 Pharmaceutical Science
摘要: A series of indeno[1,2-c]pyrazoles were discovered to be the first known inhibitors heme-regulated eukaryotic initiation factor 2alpha (HRI) kinase. The synthesis, structure-activity relationship profile, and in-vitro pharmacological characterization this inaugural HRI kinase are detailed.
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