title: Repurposing human Aurora kinase inhibitors as leads for anti-protozoan drug discovery.
abstract: Hesperadin, an established human Aurora B inhibitor, was tested against cultures ofTrypanosoma brucei, Leishmania major,andPlasmodium 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 againstT. bruceiandP. falciparumwith good selectivity. These compounds may represent an opportunity for continued optimization.
authors.affiliation: Northeastern University Department of Chemistry & Chemical Biology, 360 Huntington Avenue, Boston, MA USA. Tel: 617-373-2703.
authors.forename: Gautam
authors.initials: G
authors.lastname: Patel
authors.affiliation: Experimental Therapeutics, Walter Reed Army Institute for Research, 2460 Linden Lane, Silver Spring, MD, 20910.
authors.forename: Norma E
authors.initials: NE
authors.lastname: Roncal
authors.affiliation: Experimental Therapeutics, Walter Reed Army Institute for Research, 2460 Linden Lane, Silver Spring, MD, 20910.
authors.forename: Patricia J
authors.initials: PJ
authors.lastname: Lee
authors.affiliation: Experimental Therapeutics, Walter Reed Army Institute for Research, 2460 Linden Lane, Silver Spring, MD, 20910.
authors.forename: Susan E
authors.initials: SE
authors.lastname: Leed
authors.affiliation: Anti-Infectives Screening Core, New York University School of Medicine, New York, NY 10010.
authors.forename: Jessey
authors.initials: J
authors.lastname: Erath
authors.affiliation: New York University School of Medicine, Department of Microbiology, Division of Parasitology, 341 E. 25 St. New York, NY USA ; Anti-Infectives Screening Core, New York University School of Medicine, New York, NY 10010.
authors.forename: Ana
authors.initials: A
authors.lastname: Rodriguez
authors.affiliation: Experimental Therapeutics, Walter Reed Army Institute for Research, 2460 Linden Lane, Silver Spring, MD, 20910.
authors.forename: Richard J
authors.initials: RJ
authors.lastname: Sciotti
authors.affiliation: Northeastern University Department of Chemistry & Chemical Biology, 360 Huntington Avenue, Boston, MA USA. Tel: 617-373-2703.
authors.forename: Michael P
authors.initials: MP
authors.lastname: Pollastri