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Identification and optimization of 4-anilinoquinolines as inhibitors of cyclin G associated kinase

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 nar...

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Publication status:
Published
Peer review status:
Peer reviewed
Version:
Accepted Manuscript

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Publisher copy:
10.1002/cmdc.201700663

Authors


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Role:
Author
ORCID:
0000-0001-5871-3458
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Institution:
University of Oxford
Division:
Medical Sciences Division
Department:
NDM; Target Discovery Institute
Role:
Author
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Role:
Author
ORCID:
0000-0003-1859-3513
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Publisher:
Wiley-VCH Verlag Publisher's website
Journal:
ChemMedChem Journal website
Volume:
13
Issue:
1
Pages:
48–66
Publication date:
2017-11-27
Acceptance date:
2017-10-26
DOI:
EISSN:
1860-7187
ISSN:
1860-7179
Pubs id:
pubs:803558
URN:
uri:c872af63-724b-4860-aad8-f0f8cd9760bb
UUID:
uuid:c872af63-724b-4860-aad8-f0f8cd9760bb
Local pid:
pubs:803558
Paper number:
1

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