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; +6 more...Levy, Alison; Newman, Michelle; Taylor, Debra; Arthur, J Simon C; Clark, Kristopher; and Cohen, Philip
(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 |