| Literature DB >> 23099093 |
Edward G McIver1, 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.
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.Entities:
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Year: 2012 PMID： 23099093 DOI： 10.1016/j.bmcl.2012.09.063
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823