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Anilinoquinoline based inhibitors of trypanosomatid proliferation
JournalArticle (Originalarbeit in einer wissenschaftlichen Zeitschrift)
ID
4488635
Author(s)
Ferrins, Lori; Sharma, Amrita; Thomas, Sarah M.; Mehta, Naimee; Erath, Jessey; Tanghe, Scott; Leed, Susan E.; Rodriguez, Ana; Mensa-Wilmot, Kojo; Sciotti, Richard J.; Gillingwater, Kirsten; Pollastri, Michael P.
Anilinoquinoline based inhibitors of trypanosomatid proliferation
Journal
PLoS Neglected Tropical Diseases
Volume
12
Number
11
Pages / Article-Number
e0006834
Abstract
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.
