Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10594387 | Bioorganic & Medicinal Chemistry Letters | 2012 | 5 Pages |
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.
Keywords
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
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,