Indole-3-Carbonitriles as DYRK1A Inhibitors by Fragment-Based Drug Design

Indole-3-Carbonitriles as DYRK1A Inhibitors by Fragment-Based Drug Design

Dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) is a potential drug target because of its role in the development of Down syndrome and Alzheimer’s disease. The selective DYRK1A inhibitor 10-iodo-11H-indolo[3,2-c]quinoline-6-carboxylic acid (KuFal194), a large, flat and lipophi...

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Bibliographic Details
Main Authors: Rosanna Meine, Walter Becker, Hannes Falke, Lutz Preu, Nadège Loaëc, Laurent Meijer, Conrad Kunick
Format: Article
Language:English
Published: MDPI AG 2018-01-01
Series:Molecules
Subjects:
DYRK1A
fraction of saturation
fragment-based drug development
indole
lipophilicity
molecular docking
protein kinase inhibitor
solubility
Online Access:http://www.mdpi.com/1420-3049/23/2/64

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http://www.mdpi.com/1420-3049/23/2/64

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