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

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

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Authors

  • Edward G. McIver
  • Justin Bryans
  • Kristian Birchall
  • Jasveen Chugh
  • Thomas Drake
  • Stephen J. Lewis
  • Joanne Osborne
  • Ela Smiljanic-Hurley
  • William Tsang
  • Ahmad Kamal
  • Alison Levy
  • Michelle Newman
  • Debra Taylor
  • J. Simon C. Arthur
  • Kristopher Clark
  • Philip Cohen

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Info

Original languageEnglish
Pages7169-7173
Number of pages5
JournalBioorganic & Medicinal Chemistry Letters
Journal publication date2012
Journal number23
Volume22
DOIs
StatePublished

Abstract

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.

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