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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.

Original publication

DOI

10.1002/cmdc.201700663

Type

Journal article

Journal

ChemMedChem

Publication Date

08/01/2018

Volume

13

Pages

48 - 66

Keywords

anilinoquinolines, antibacterial agents, chemical probes, cyclin G associated kinase (GAK)