Repurposing human Aurora kinase inhibitors as leads for anti-protozoan drug discovery?

MedChemComm Pub Date: 2014-03-17 DOI: 10.1039/C4MD00045E

Abstract

Hesperadin, an established human Aurora B inhibitor, was tested against cultures of Trypanosoma brucei, Leishmania major, and Plasmodium falciparum, and was identified to be a potent proliferation inhibitor. A series of analogs was designed and tested to establish the initial structure–activity relationships for each parasite. In this study, we identified multiple non-toxic compounds with high potency against T. brucei and P. falciparum with good selectivity. These compounds may represent an opportunity for continued optimization.

Graphical abstract: Repurposing human Aurora kinase inhibitors as leads for anti-protozoan drug discovery
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