Literature DB >> 29072804

Identification and Optimization of 4-Anilinoquinolines as Inhibitors of Cyclin G Associated Kinase.

Christopher R M Asquith1, Tuomo Laitinen2, James M Bennett3, Paulo H Godoi4, Michael P East5, Graham J Tizzard6, Lee M Graves5, Gary L Johnson5, Ronna E Dornsife1, Carrow I Wells1, Jonathan M Elkins3,4, Timothy M Willson1, William J Zuercher1.   

Abstract

4-Anilinoquinolines were identified as potent and narrow-spectrum inhibitors of the cyclin G associated kinase (GAK), an important regulator of viral and bacterial entry into host cells. Optimization of the 4-anilino group and the 6,7-quinoline substituents produced GAK inhibitors with nanomolar activity, over 50 000-fold selectivity relative to other members of the numb-associated kinase (NAK) subfamily, and a compound (6,7-dimethoxy-N-(3,4,5-trimethoxyphenyl)quinolin-4-amine; 49) with a narrow-spectrum kinome profile. These compounds may be useful tools to explore the therapeutic potential of GAK in prevention of a broad range of infectious and systemic diseases.
© 2018 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.

Entities:  

Keywords:  anilinoquinolines; antibacterial agents; chemical probes; cyclin G associated kinase (GAK)

Mesh：

Substances：

Year:  2017        PMID： 29072804      PMCID： PMC5914168          DOI： 10.1002/cmdc.201700663

Source DB:  PubMed          Journal:  ChemMedChem        ISSN： 1860-7179            Impact factor:   3.466


  51 in total

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Journal:  Nat Commun       Date:  2015-12-03       Impact factor: 14.919
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  15 in total

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2.  Optimization of Isothiazolo[4,3- b]pyridine-Based Inhibitors of Cyclin G Associated Kinase (GAK) with Broad-Spectrum Antiviral Activity.

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4.  Identification of 4-Anilinoquin(az)oline as a Cell-Active Protein Kinase Novel 3 (PKN3) Inhibitor Chemotype.

Authors:  Christopher R M Asquith; Louisa Temme; Michael P East; Tuomo Laitinen; Julie Pickett; Frank E Kwarcinski; Parvathi Sinha; Carrow I Wells; Gary L Johnson; Reena Zutshi; David H Drewry
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5.  Anti-tubercular activity of novel 4-anilinoquinolines and 4-anilinoquinazolines.

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6.  SGC-AAK1-1: A Chemical Probe Targeting AAK1 and BMP2K.

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7.  New Insights into 4-Anilinoquinazolines as Inhibitors of Cardiac Troponin I-Interacting Kinase (TNNi3K).

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Review 8.  Medicinal chemistry strategies toward host targeting antiviral agents.

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Journal:  Cell Rep       Date:  2019-01-02       Impact factor: 9.423
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