Design, Synthesis and Biological Evaluation of Isoxazole-Based CK1 Inhibitors Modified with Chiral Pyrrolidine Scaffolds

Design, Synthesis and Biological Evaluation of Isoxazole-Based CK1 Inhibitors Modified with Chiral Pyrrolidine Scaffolds

In this study, we report on the modification of a 3,4-diaryl-isoxazole-based CK1 inhibitor with chiral pyrrolidine scaffolds to develop potent and selective CK1 inhibitors. The pharmacophore of the lead structure was extended towards the ribose pocket of the adenosine triphosphate (ATP) binding site...

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Bibliographic Details
Main Authors: Andreas Luxenburger, Dorian Schmidt, Chiara Ianes, Christian Pichlo, Marc Krüger, Thorsten von Drathen, Elena Brunstein, Graeme J. Gainsford, Ulrich Baumann, Uwe Knippschild, Christian Peifer
Format: Article
Language:English
Published: MDPI AG 2019-03-01
Series:Molecules
Subjects:
protein kinase CK1
formerly known as casein kinase 1
chiral kinase inhibitors
iminoribitol
ribose pocket
3,4-diaryl-isoxazole
Pictet-Spengler cyclization
Online Access:http://www.mdpi.com/1420-3049/24/5/873

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