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

Abstract

Hesperadin, an established human Aurora B inhibitor, was tested against cultures of <i>Trypanosoma brucei, Leishmania major,</i> and <i>Plasmodium falciparum,</i> 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 <i>T. brucei</i> and <i>P. falciparum</i> with good selectivity. These compounds may represent an opportunity for continued optimization.