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Synthesis and structure-activity relationships of a novel series of pyrimidines as potent inhibitors of TBK1/IKKε kinases

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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; Levy, Alison; Newman, Michelle; Taylor, Debra; 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 journalArticle

Harvard

McIver, EG, Bryans, J, Birchall, K, Chugh, J, Drake, T, Lewis, SJ, Osborne, J, Smiljanic-Hurley, E, Tsang, W, Kamal, A, Levy, A, Newman, M, Taylor, D, Arthur, JSC, Clark, K & Cohen, P 2012, 'Synthesis and structure-activity relationships of a novel series of pyrimidines as potent inhibitors of TBK1/IKKε kinases' Bioorganic & Medicinal Chemistry Letters, vol 22, no. 23, pp. 7169-7173., 10.1016/j.bmcl.2012.09.063

APA

McIver, E. G., Bryans, J., Birchall, K., Chugh, J., Drake, T., Lewis, S. J., ... Cohen, P. (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), 7169-7173. 10.1016/j.bmcl.2012.09.063

Vancouver

McIver EG, Bryans J, Birchall K, Chugh J, Drake T, Lewis SJ et al. Synthesis and structure-activity relationships of a novel series of pyrimidines as potent inhibitors of TBK1/IKKε kinases. Bioorganic & Medicinal Chemistry Letters. 2012 Dec;22(23):7169-7173. Available from: 10.1016/j.bmcl.2012.09.063

Author

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

In: Bioorganic & Medicinal Chemistry Letters, Vol. 22, No. 23, 12.2012, p. 7169-7173.

Research output: Contribution to journalArticle

Bibtex - Download

@article{112a445aceab461eb806ca2451bc2fc3,
title = "Synthesis and structure-activity relationships of a novel series of pyrimidines as potent inhibitors of TBK1/IKKε kinases",
author = "McIver, {Edward G.} and Justin Bryans and Kristian Birchall and Jasveen Chugh and Thomas Drake and Lewis, {Stephen J.} and Joanne Osborne and Ela Smiljanic-Hurley and William Tsang and Ahmad Kamal and Alison Levy and Michelle Newman and Debra Taylor and Arthur, {J. Simon C.} and Kristopher Clark and Philip Cohen",
year = "2012",
doi = "10.1016/j.bmcl.2012.09.063",
volume = "22",
number = "23",
pages = "7169--7173",
journal = "Bioorganic & Medicinal Chemistry Letters",
issn = "0960-894X",

}

RIS (suitable for import to EndNote) - Download

TY - JOUR

T1 - Synthesis and structure-activity relationships of a novel series of pyrimidines as potent inhibitors of TBK1/IKKε kinases

A1 - McIver,Edward G.

A1 - Bryans,Justin

A1 - Birchall,Kristian

A1 - Chugh,Jasveen

A1 - Drake,Thomas

A1 - Lewis,Stephen J.

A1 - Osborne,Joanne

A1 - Smiljanic-Hurley,Ela

A1 - Tsang,William

A1 - Kamal,Ahmad

A1 - Levy,Alison

A1 - Newman,Michelle

A1 - Taylor,Debra

A1 - Arthur,J. Simon C.

A1 - Clark,Kristopher

A1 - Cohen,Philip

AU - McIver,Edward G.

AU - Bryans,Justin

AU - Birchall,Kristian

AU - Chugh,Jasveen

AU - Drake,Thomas

AU - Lewis,Stephen J.

AU - Osborne,Joanne

AU - Smiljanic-Hurley,Ela

AU - Tsang,William

AU - Kamal,Ahmad

AU - Levy,Alison

AU - Newman,Michelle

AU - Taylor,Debra

AU - Arthur,J. Simon C.

AU - Clark,Kristopher

AU - Cohen,Philip

PY - 2012/12

Y1 - 2012/12

N2 - <p>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.</p>

AB - <p>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.</p>

UR - http://www.scopus.com/inward/record.url?scp=84867608938&partnerID=8YFLogxK

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 -

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