Kinase scaffold repurposing for neglected disease drug discovery: Discovery of an efficacious, lapatanib-derived lead compound for trypanosomiasis

…, P Edwards, NE Roncal, K Mensa-Wilmot…

Index: Patel, Gautam; Karver, Caitlin E.; Behera, Ranjan; Guyett, Paul J.; Sullenberger, Catherine; Edwards, Peter; Roncal, Norma E.; Mensa-Wilmot, Kojo; Pollastri, Michael P. Journal of Medicinal Chemistry, 2013 , vol. 56, # 10 p. 3820 - 3832

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Citation Number: 34

Abstract

Human African trypanosomiasis (HAT) is a neglected tropical disease caused by the protozoan parasite Trypanosoma brucei. Because drugs in use against HAT are toxic and require intravenous dosing, new drugs are needed. Initiating lead discovery campaigns by using chemical scaffolds from drugs approved for other indications can speed up drug discovery for neglected diseases. We demonstrated recently that the 4- ...