Back Cover: From On‐Target to Off‐Target Activity: Identification and Optimisation of Trypanosoma brucei GSK3 Inhibitors and Their Characterisation as Anti‐Trypanosoma brucei Drug Discovery Lead Molecules (ChemMedChem 7/2013). Issue 7 (26th June 2013)

• Record Type: Journal Article
• Authors: Woodland, Andrew; Grimaldi, Raffaella; Luksch, Torsten; Cleghorn, Laura A. T.; Ojo, Kayode K.; Van Voorhis, Wesley C.; Brenk, Ruth; Frearson, Julie A.; Gilbert, Ian H.; Wyatt, Paul G.
• Is Part Of: ChemMedChem. Volume 8:Issue 7(2013:Jul.)
• Page Start: 1228
• Page End: 1228
• Publication Date: 2013-06-26
• Subjects: Pharmaceutical chemistry -- Periodicals; 615.19005
• DOI: 10.1002/cmdc.201390029
• Languages: English
• ISSNs: 1860-7179

Abstract

<abstract abstract-type="graphical" xml:lang="en"> <title> <x xml:space="preserve">Abstract</x> </title> <p> <bold>The back cover picture shows</bold> the discovery of <italic>Trypanosoma brucei</italic> protein kinase GSK3 short (<italic>Tb</italic>GSK3) inhibitors and their characterization as leads in the development of novel therapeutics against Human African trypanosomiasis (HAT). Hit validation and optimization gave rise to a series of diaminothiazoles with low nanomolar activities against <italic>Tb</italic>GSK3 that are potent in vitro inhibitors of <italic>T. brucei</italic> proliferation. For more details, see the Full Paper by Ian H. Gilbert, Paul G. Wyatt et al. on <ext-link ext-link-type="doi" xlink:type="simple" xmlns:xlink="http://www.w3.org/1999/xlink">p. 1127 ff.</ext-link><boxed-text content-type="graphic" position="anchor" orientation="portrait"><graphic position="anchor" mimetype="image" xlink:href="ark:/27927/pgg22f67qmp" orientation="portrait" xlink:type="simple" xmlns:xlink="http://www.w3.org/1999/xlink" /></boxed-text></p> </abstract>