3-Aryl-4-(arylhydrazono)-1H-pyrazol-5-ones: Highly ligand efficient and potent inhibitors of GSK3b

A series of 3-aryl-4-(arylhydrazono)-1H-pyrazol-5-one inhibitors of GSK3b was developed from a low molecular weight, highly ligand efficient screening hit 1. Hit-to-lead optimization led to a number of highly potent inhibitors, while maintaining the high ligand efficiency of the screening hit. AB:

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2010-03, Vol.20 (5), p.1661-1664
Main Authors: Arnost, Michael, Pierce, Al, Ter Haar, Ernst, Lauffer, David, Madden, Jaren, Tanner, Kirk, Green, Jeremy
Format: Article
Language:English
Online Access:Get full text
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Description
Summary:A series of 3-aryl-4-(arylhydrazono)-1H-pyrazol-5-one inhibitors of GSK3b was developed from a low molecular weight, highly ligand efficient screening hit 1. Hit-to-lead optimization led to a number of highly potent inhibitors, while maintaining the high ligand efficiency of the screening hit. AB:
ISSN:0960-894X
DOI:10.1016/j.bmcl.2010.01.072