Discovery of the first known small-molecule inhibitors of heme-regulated eukaryotic initiation factor 2α (HRI) kinase

Mark D. Rosen,Craig R. Woods,Steven D. Goldberg,Michael D. Hack,A. Dawn Bounds,Young Yang,Pamela C. Wagaman,Victor K. Phuong,Angela P. Ameriks,Terrance D. Barrett,Kimon C. Kanelakis,Jui Chang,Nigel P. Shankley,Michael H. Rabinowitz

Bioorganic & Medicinal Chemistry Letters（2009）

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摘要

A series of indeno[1,2-c]pyrazoles were discovered to be the first known inhibitors of heme-regulated eukaryotic initiation factor 2α (HRI) kinase. The synthesis, structure–activity relationship profile, and in-vitro pharmacological characterization of this inaugural series of HRI kinase inhibitors are detailed.

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关键词

Anemia,Kinase inhibitors,Hemoglobin,HRI kinase,Blood

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