Literature DB >> 21764580

Identification of 2-(4-pyridyl)thienopyridinones as GSK-3β inhibitors.

Gabriella Gentile1, Giovanni Bernasconi, Alfonso Pozzan, Giancarlo Merlo, Paola Marzorati, Paul Bamborough, Benjamin Bax, Angela Bridges, Caroline Brough, Paul Carter, Geoffrey Cutler, Margarete Neu, Mia Takada.   

Abstract

The discovery of a novel series of 2-(4-pyridyl)thienopyridinone GSK-3β inhibitors is reported. X-ray crystallography reveals its binding mode and enables rationalization of the SAR. The initial optimization of the template for improved cellular activity and predicted CNS penetration is also presented.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID: 21764580     DOI: 10.1016/j.bmcl.2011.06.050

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


  3 in total

1.  Photooxygenation of an amino-thienopyridone yields a more potent PTP4A3 inhibitor.

Authors:  Joseph M Salamoun; Kelley E McQueeney; Kalyani Patil; Steven J Geib; Elizabeth R Sharlow; John S Lazo; Peter Wipf
Journal:  Org Biomol Chem       Date:  2016-07-06       Impact factor: 3.876

2.  N-terminal phosphorylation regulates the activity of glycogen synthase kinase 3 from Plasmodium falciparum.

Authors:  Samuel Pazicky; Arne Alder; Haydyn Mertens; Dmitri Svergun; Tim Gilberger; Christian Löw
Journal:  Biochem J       Date:  2022-02-11       Impact factor: 3.857

3.  Discovery of Novel Antiangiogenic Marine Natural Product Scaffolds.

Authors:  Hassan Y Ebrahim; Khalid A El Sayed
Journal:  Mar Drugs       Date:  2016-03-11       Impact factor: 5.118

  3 in total

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