Literature DB >> 16460937

Synthesis and evaluation of novel heterocyclic inhibitors of GSK-3.

Terrence L Smalley1, Andrew J Peat, Joyce A Boucheron, Scott Dickerson, Dulce Garrido, Frank Preugschat, Stephanie L Schweiker, Stephen A Thomson, Tony Y Wang.   

Abstract

A set of novel heterocyclic pyrimidyl hydrazones has been synthesized as inhibitors of glycogen synthase kinase-3 (GSK-3) with the most active exhibiting low nanomolar activity. Quantum mechanical calculations indicate that of the conformational factors that could determine binding affinity, the planarity of the phenyl ring in relation to the central core and the conformation of the hydrazone chain may be the most influential.

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Year:  2006        PMID: 16460937     DOI: 10.1016/j.bmcl.2006.01.057

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


  8 in total

1.  Synthesis and Initial in Vivo Studies with [(11)C]SB-216763: The First Radiolabeled Brain Penetrative Inhibitor of GSK-3.

Authors:  Lei Li; Xia Shao; Erin L Cole; Stephan A Ohnmacht; Valentina Ferrari; Young T Hong; David J Williamson; Tim D Fryer; Carole A Quesada; Phillip Sherman; Patrick J Riss; Peter J H Scott; Franklin I Aigbirhio
Journal:  ACS Med Chem Lett       Date:  2015-03-10       Impact factor: 4.345

2.  Design, Synthesis, and Antitumor Evaluation of Novel Pyrazolo[3,4-d]pyrimidine Derivatives.

Authors:  Manal M Kandeel; Lamia W Mohamed; Mohammed K Abd El Hamid; Ahmed T Negmeldin
Journal:  Sci Pharm       Date:  2012-06-25

3.  N-N bond-forming cyclization for the one-pot synthesis of N-aryl[3,4-d]pyrazolopyrimidines.

Authors:  Lindsay E Evans; Matthew D Cheeseman; Keith Jones
Journal:  Org Lett       Date:  2012-06-26       Impact factor: 6.005

4.  1-{(E)-[5-(2-Nitro-phen-yl)furan-2-yl]methyl-idene}-2,2-diphenyl-hydrazine.

Authors:  Marcos Flores-Alamo; Blanca M Cabrera-Vivas; Ruth Meléndrez-Luevano; Julio M Hernández P; Lena Ruiz-Azuara
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2012-12-15

5.  Syntheses, spectral characterization, and antimicrobial studies on the coordination compounds of metal ions with schiff base containing both aliphatic and aromatic hydrazide moieties.

Authors:  Dinesh Kumar; Silky Chadda; Jyoti Sharma; Parveen Surain
Journal:  Bioinorg Chem Appl       Date:  2013-10-03       Impact factor: 7.778

6.  Crystal structure of (E)-1-(2-nitro-benzyl-idene)-2,2-di-phenyl-hydrazine.

Authors:  Marcos Flores-Alamo; Ruth Meléndrez-Luévano; José A Ortiz Márquez; Estibaliz Sansinenea Royano; Blanca M Cabrera-Vivas
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2014-08-01

Review 7.  Glycogen Synthase Kinase-3 (GSK-3)-Targeted Therapy and Imaging.

Authors:  Mukesh K Pandey; Timothy R DeGrado
Journal:  Theranostics       Date:  2016-02-17       Impact factor: 11.556

8.  Crystal Structure and Inhibitor Identifications Reveal Targeting Opportunity for the Atypical MAPK Kinase ERK3.

Authors:  Martin Schröder; Panagis Filippakopoulos; Martin P Schwalm; Carla A Ferrer; David H Drewry; Stefan Knapp; Apirat Chaikuad
Journal:  Int J Mol Sci       Date:  2020-10-26       Impact factor: 5.923

  8 in total

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