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Methyl 9-anilinothiazolo[5,4-f]quinazoline-2-carbimidates 1 (EHT 5372) and 2 (EHT 1610) are strong inhibitors of DYRK's family kinases. The crystal structures of the complex revealed a noncanonical binding mode of compounds 1 and 2 in DYRK2, explaining the remarkable selectivity and potency of these inhibitors. The structural data and comparison presented here provide therefore a template for further improvement of this inhibitor class and for the development of novel inhibitors selectively targeting DYRK kinases.

Original publication

DOI

10.1021/acs.jmedchem.6b01083

Type

Journal article

Journal

J Med Chem

Publication Date

23/11/2016

Volume

59

Pages

10315 - 10321

Keywords

Dose-Response Relationship, Drug, Humans, Models, Molecular, Molecular Structure, Phosphorylation, Protein Kinase Inhibitors, Protein-Tyrosine Kinases, Quinazolines, Structure-Activity Relationship