Article
Discovery of Inhibitors of Trypanosoma brucei by Phenotypic Screening of a Focused Protein Kinase Library.
ChemMedChem - 1 Nov 2015
Woodland Andrew, Thompson Stephen, Cleghorn Laura A T, Norcross Neil, De Rycker Manu, Grimaldi Raffaella, Hallyburton Irene, Rao Bhavya, Norval Suzanne, Stojanovski Laste, Brun Reto, Kaiser Marcel, Frearson Julie A, Gray David W, Wyatt Paul G, Read Kevin D, Gilbert Ian H
Abstract excerpt
A screen of a focused kinase inhibitor library against Trypanosoma brucei rhodesiense led to the identification of seven series, totaling 121 compounds, which showed >50 % inhibition at 5 μm. Screening of these hits in a T. b. brucei proliferation assay highlighted three compounds with a 1H-imidazo[4,5-b]pyrazin-2(3H)-one scaffold that showed sub-micromolar activity and excellent selectivity against the MRC5 cell...
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