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I04-1-Macromolecular Crystallography (fixed wavelength)	[b]-Annulated halogen-substituted indoles as potential DYRK1A inhibitors Christian Lechner , Maren Flaßhoff , Hannes Falke , Lutz Preu , Nadége Loaëc , Laurent Meijer , Stefan Knapp , Apirat Chaikuad , Conrad Kunick Molecules 24 DOI: 10.3390/molecules24224090 Diamond Proposal Number(s): [8421] Open Access Show Abstract ▼ Abstract: Since hyperactivity of the protein kinase DYRK1A is linked to several neurodegenerative disorders, DYRK1A inhibitors have been suggested as potential therapeutics for Down syndrome and Alzheimer’s disease. Most published inhibitors to date suffer from low selectivity against related kinases or from unfavorable physicochemical properties. In order to identify DYRK1A inhibitors with improved properties, a series of new chemicals based on [b]-annulated halogenated indoles were designed, synthesized, and evaluated for biological activity. Analysis of crystal structures revealed a typical type-I binding mode of the new inhibitor 4-chlorocyclohepta[b]indol-10(5H)-one in DYRK1A, exploiting mainly shape complementarity for tight binding. Conversion of the DYRK1A inhibitor 8-chloro-1,2,3,9-tetrahydro-4H-carbazol-4-one into a corresponding Mannich base hydrochloride improved the aqueous solubility but abrogated kinase inhibitory activity.	Nov 2019

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