| Literature DB >> 22305584 |
Tao Wang1, Michael A Block, Scott Cowen, Audrey M Davies, Erik Devereaux, Lakshmaiah Gingipalli, Jeffrey Johannes, Nicholas A Larsen, Qibin Su, Julie A Tucker, David Whitston, Jiaquan Wu, Hai-Jun Zhang, Michael Zinda, Claudio Chuaqui.
Abstract
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. 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 IKKε.Entities:
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Year: 2012 PMID： 22305584 DOI： 10.1016/j.bmcl.2012.01.018
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823