Synthesis and structure-activity relationships of a novel series of pyrimidines as potent inhibitors of TBK1/IKKε kinases.
McIver, EG; Bryans, J; Birchall, K; Chugh, J; Drake, T; Lewis, SJ; Osborne, J; Smiljanic-Hurley, E; Tsang, W; Kamal, A; +6 more...Levy, A; Newman, M; Taylor, D; Arthur, JSC; Clark, K; Cohen, P and
(2012)
Synthesis and structure-activity relationships of a novel series of pyrimidines as potent inhibitors of TBK1/IKKε kinases.
Bioorganic & medicinal chemistry letters, 22 (23).
pp. 7169-7173.
ISSN 0960-894X
DOI: 10.1016/j.bmcl.2012.09.063
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.
| Item Type | Article |
|---|---|
| ISI | 310583100036 |
| Date Deposited | 18 Jul 2017 01:03 |