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Anilinoquinoline based inhibitors of trypanosomatid proliferation
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...
Autores principales: | , , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Public Library of Science
2018
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6283615/ https://www.ncbi.nlm.nih.gov/pubmed/30475800 http://dx.doi.org/10.1371/journal.pntd.0006834 |
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author | 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. |
author_facet | 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. |
author_sort | Ferrins, Lori |
collection | PubMed |
description | 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. |
format | Online Article Text |
id | pubmed-6283615 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2018 |
publisher | Public Library of Science |
record_format | MEDLINE/PubMed |
spelling | pubmed-62836152018-12-19 Anilinoquinoline based inhibitors of trypanosomatid proliferation 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. PLoS Negl Trop Dis Research Article 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. Public Library of Science 2018-11-26 /pmc/articles/PMC6283615/ /pubmed/30475800 http://dx.doi.org/10.1371/journal.pntd.0006834 Text en https://creativecommons.org/publicdomain/zero/1.0/ This is an open access article, free of all copyright, and may be freely reproduced, distributed, transmitted, modified, built upon, or otherwise used by anyone for any lawful purpose. The work is made available under the Creative Commons CC0 (https://creativecommons.org/publicdomain/zero/1.0/) public domain dedication. |
spellingShingle | Research Article 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 |
title | Anilinoquinoline based inhibitors of trypanosomatid proliferation |
title_full | Anilinoquinoline based inhibitors of trypanosomatid proliferation |
title_fullStr | Anilinoquinoline based inhibitors of trypanosomatid proliferation |
title_full_unstemmed | Anilinoquinoline based inhibitors of trypanosomatid proliferation |
title_short | Anilinoquinoline based inhibitors of trypanosomatid proliferation |
title_sort | anilinoquinoline based inhibitors of trypanosomatid proliferation |
topic | Research Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6283615/ https://www.ncbi.nlm.nih.gov/pubmed/30475800 http://dx.doi.org/10.1371/journal.pntd.0006834 |
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