Discovery of azabenzimidazole derivatives as potent, selective inhibitors of TBK1/IKKε kinases.


The design, synthesis and biological evaluation of a series of azabenzimidazole derivatives as TBK1/IKKε kinase inhibitors are described. Starting from a lead compound 1a, iterative design and SAR exploitation of the scaffold led to analogues with nM enzyme potencies against TBK1/IKKε. These compounds also exhibited excellent cellular activity against TBK1… (More)
DOI: 10.1016/j.bmcl.2012.01.018


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