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


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, JS; 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, 22 (23). pp. 7169-73. ISSN 0960-894X DOI: https://doi.org/10.1016/j.bmcl.2012.09.063

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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/IKKε pathway in inflammatory diseases.

Item Type: Article
Faculty and Department: Faculty of Public Health and Policy > Dept of Global Health and Development
PubMed ID: 23099093
Web of Science ID: 310583100036
URI: http://researchonline.lshtm.ac.uk/id/eprint/4086849

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