Synthesis and structure-activity relationships of a novel series of pyrimidines as potent inhibitors of TBK1/IKKε kinases. / McIver, E.G.; Bryans, J.; Birchall, K.; Chugh, J.; Drake, T.; Lewis, S.J.; Osborne, J.; Smiljanic-Hurley, E.; Tsang, W.; Kamal, A.; Levy, A.; Newman, M.; Taylor, D.; Arthur, J.Simon C.; Clark, Kristopher; Cohen, Philip.
In: Bioorganic & Medicinal Chemistry Letters, Vol. 22, No. 23, 12.2012, p. 7169-7173.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Synthesis and structure-activity relationships of a novel series of pyrimidines as potent inhibitors of TBK1/IKKε kinases
A1 - McIver,E.G.
A1 - Bryans,J.
A1 - Birchall,K.
A1 - Chugh,J.
A1 - Drake,T.
A1 - Lewis,S.J.
A1 - Osborne,J.
A1 - Smiljanic-Hurley,E.
A1 - Tsang,W.
A1 - Kamal,A.
A1 - Levy,A.
A1 - Newman,M.
A1 - Taylor,D.
A1 - Arthur,J.Simon C.
A1 - Clark,Kristopher
A1 - Cohen,Philip
AU - McIver,E.G.
AU - Bryans,J.
AU - Birchall,K.
AU - Chugh,J.
AU - Drake,T.
AU - Lewis,S.J.
AU - Osborne,J.
AU - Smiljanic-Hurley,E.
AU - Tsang,W.
AU - Kamal,A.
AU - Levy,A.
AU - Newman,M.
AU - Taylor,D.
AU - Arthur,J.Simon C.
AU - Clark,Kristopher
AU - Cohen,Philip
PY - 2012/12
Y1 - 2012/12
N2 - 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/IKKe pathway in inflammatory diseases. © 2012 Elsevier Ltd. All rights reserved.
AB - 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/IKKe pathway in inflammatory diseases. © 2012 Elsevier Ltd. All rights reserved.
UR - http://www.scopus.com/inward/record.url?partnerID=yv4JPVwI&eid=2-s2.0-84867608938&md5=6b38ac1716ca4560195a81f0e2352371
U2 - 10.1016/j.bmcl.2012.09.063
DO - 10.1016/j.bmcl.2012.09.063
M1 - Article
JO - Bioorganic & Medicinal Chemistry Letters
JF - Bioorganic & Medicinal Chemistry Letters
SN - 0960-894X
IS - 23
VL - 22
SP - 7169
EP - 7173
ER -