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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 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.

SUBMITTER: Patel G

PROVIDER: S-EPMC4045489 | biostudies-other | 2014 May

REPOSITORIES: biostudies-other

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

Patel Gautam G Roncal Norma E NE Lee Patricia J PJ Leed Susan E SE Erath Jessey J Rodriguez Ana A Sciotti Richard J RJ Pollastri Michael P MP

MedChemComm 20140501 5

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 co ...[more]

PMID: 24910766

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