Literature DB >> 20138514

3-Aryl-4-(arylhydrazono)-1H-pyrazol-5-ones: Highly ligand efficient and potent inhibitors of GSK3beta.

Michael Arnost1, Al Pierce, Ernst ter Haar, David Lauffer, Jaren Madden, Kirk Tanner, Jeremy Green.   

Abstract

A series of 3-aryl-4-(arylhydrazono)-1H-pyrazol-5-one inhibitors of GSK3beta 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. Copyright 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID: 20138514     DOI: 10.1016/j.bmcl.2010.01.072

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  5 in total

1.  A second polymorph of (Z)-3-amino-4-(2-phenyl-hydrazinyl-idene)-1H-pyrazol-5(4H)-one.

Authors:  Abdel-Sattar S Hamad Elgazwy; Peter G Jones
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2014-01-15

2.  Designing of dual inhibitors for GSK-3β and CDK5: Virtual screening and in vitro biological activities study.

Authors:  Hongbo Xie; Haixia Wen; Denan Zhang; Lei Liu; Bo Liu; Qiuqi Liu; Qing Jin; Kehui Ke; Ming Hu; Xiujie Chen
Journal:  Oncotarget       Date:  2017-03-14

3.  Small-Molecule Inhibitors of GSK-3: Structural Insights and Their Application to Alzheimer's Disease Models.

Authors:  Thomas Kramer; Boris Schmidt; Fabio Lo Monte
Journal:  Int J Alzheimers Dis       Date:  2012-07-22

4.  Strong nonadditivity as a key structure-activity relationship feature: distinguishing structural changes from assay artifacts.

Authors:  Christian Kramer; Julian E Fuchs; Klaus R Liedl
Journal:  J Chem Inf Model       Date:  2015-03-11       Impact factor: 4.956

5.  Computer-aided molecular design of pyrazolotriazines targeting glycogen synthase kinase 3.

Authors:  M Lourdes Sciú; Victor Sebastián-Pérez; Loreto Martinez-Gonzalez; Rocio Benitez; Daniel I Perez; Concepción Pérez; Nuria E Campillo; Ana Martinez; E Laura Moyano
Journal:  J Enzyme Inhib Med Chem       Date:  2019-12       Impact factor: 5.051

  5 in total

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