1365645-31-3Relevant articles and documents
Discovery of azabenzimidazole derivatives as potent, selective inhibitors of TBK1/IKK kinases
Wang, Tao,Block, Michael A.,Cowen, Scott,Davies, Audrey M.,Devereaux, Erik,Gingipalli, Lakshmaiah,Johannes, Jeffrey,Larsen, Nicholas A.,Su, Qibin,Tucker, Julie A.,Whitston, David,Wu, Jiaquan,Zhang, Hai-Jun,Zinda, Michael,Chuaqui, Claudio
, p. 2063 - 2069 (2012)
The design, synthesis and biological evaluation of a series of azabenzimidazole derivatives as TBK1/IKK 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/IKK. These compounds also exhibited excellent cellular activity against TBK1. Further structure-based design to improve selectivity over CDK2 and Aurora B resulted in compounds such as 5b-e. These probe compounds will facilitate study of the complex cancer biology of TBK1 and IKK.
