Synthesis and structure-activity relationships of a novel series of pyrimidines as potent inhibitors of TBK1/IKKε kinases.
Edward G McIver;
Justin Bryans;
Kristian Birchall;
Jasveen Chugh;
Thomas Drake;
Stephen J Lewis;
Joanne Osborne;
Ela Smiljanic-Hurley;
William Tsang;
Ahmad Kamal;
+6 more...
Alison Levy;
Michelle Newman;
Debra Taylor;
J Simon C Arthur;
Kristopher Clark;
Philip Cohen;
(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 |