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 |
| Date Deposited | 18 Jul 2017 01:03 |