Anilinoquinoline based inhibitors of trypanosomatid proliferation.

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.

journal_name

PLoS Negl Trop Dis

authors

Ferrins L,Sharma A,Thomas SM,Mehta N,Erath J,Tanghe S,Leed SE,Rodriguez A,Mensa-Wilmot K,Sciotti RJ,Gillingwater K,Pollastri MP

doi

10.1371/journal.pntd.0006834

subject

Has Abstract

pub_date

2018-11-26 00:00:00

pages

e0006834

issue

11

eissn

1935-2727

issn

1935-2735

pii

PNTD-D-18-00885

journal_volume

12

pub_type

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