Anilinoquinoline based inhibitors of trypanosomatid proliferation

Ferrins, Lori and Sharma, Amrita and Thomas, Sarah M. and Mehta, Naimee and Erath, Jessey and Tanghe, Scott and Leed, Susan E. and Rodriguez, Ana and Mensa-Wilmot, Kojo and Sciotti, Richard J. and Gillingwater, Kirsten and Pollastri, Michael P.. (2018) Anilinoquinoline based inhibitors of trypanosomatid proliferation. PLoS Neglected Tropical Diseases, 12 (11). e0006834.

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We recently reported the medicinal chemistry re-optimization of a series of compounds derived from the human tyrosine kinase inhibitor, lapatinib, for activity against Plasmodium falciparum. From this same library of compounds, we now report potent compounds against Trypanosoma brucei brucei (which causes human African trypanosomiasis), T. cruzi (the pathogen that causes Chagas disease), and Leishmania spp. (which cause leishmaniasis). In addition, sub-micromolar compounds were identified that inhibit proliferation of the parasites that cause African animal trypanosomiasis, T. congolense and T. vivax. We have found that this set of compounds display acceptable physicochemical properties and represent progress towards identification of lead compounds to combat several neglected tropical diseases.
Faculties and Departments:09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH)
09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH) > Department of Medical Parasitology and Infection Biology (MPI) > Parasite Chemotherapy (Mäser)
UniBasel Contributors:Gillingwater, Kirsten
Item Type:Article, refereed
Article Subtype:Research Article
Publisher:Public Library of Science
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:17 Dec 2018 09:00
Deposited On:17 Dec 2018 09:00

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