Synthesis and structure-activity relationships of a novel series of pyrimidines as potent inhibitors of TBK1/IKKε kinases.
- McIver, Edward G
- Bryans, Justin
- Birchall, Kristian
- Chugh, Jasveen
- Drake, Thomas
- Lewis, Stephen J
- Osborne, Joanne
- Smiljanic-Hurley, Ela
- Tsang, William
- Kamal, Ahmad
- Levy, Alison
- Newman, Michelle
- Taylor, Debra
- Arthur, J Simon C
- Clark, Kristopher
- Cohen, Philip
DOIAbstract
The design, synthesis and structure-activity relationships of a novel series of 2,4-diamino-5-cyclopropyl pyrimidines is described. Starting from BX795, originally reported to be a potent inhibitor of PDK1, we have developed compounds with improved selectivity and drug-like properties. These compounds have been evaluated in a range of cellular and in vivo assays, enabling us to probe the putative role of the TBK1/IKKε pathway in inflammatory diseases
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