Structure–Bioactivity Relationships of Lapatinib Derived Analogs against Schistosoma mansoni

[Image: see text] We recently reported a series of compounds for a solubility-driven optimization campaign of antitrypanosomal compounds. Extending a parasite-hopping approach to the series, a subset of compounds from this library has been cross-screened for activity against the metazoan flatworm pa...

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Autores principales: Buskes, Melissa J., Clements, Monica, Bachovchin, Kelly A., Jalani, Hitesh B., Leonard, Allison, Bag, Seema, Klug, Dana M., Singh, Baljinder, Campbell, Robert F., Sciotti, Richard J., El-Sakkary, Nelly, Caffrey, Conor R., Pollastri, Michael P., Ferrins, Lori
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2020
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7073886/
https://www.ncbi.nlm.nih.gov/pubmed/32184954
http://dx.doi.org/10.1021/acsmedchemlett.9b00455
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author Buskes, Melissa J.
Clements, Monica
Bachovchin, Kelly A.
Jalani, Hitesh B.
Leonard, Allison
Bag, Seema
Klug, Dana M.
Singh, Baljinder
Campbell, Robert F.
Sciotti, Richard J.
El-Sakkary, Nelly
Caffrey, Conor R.
Pollastri, Michael P.
Ferrins, Lori
author_facet Buskes, Melissa J.
Clements, Monica
Bachovchin, Kelly A.
Jalani, Hitesh B.
Leonard, Allison
Bag, Seema
Klug, Dana M.
Singh, Baljinder
Campbell, Robert F.
Sciotti, Richard J.
El-Sakkary, Nelly
Caffrey, Conor R.
Pollastri, Michael P.
Ferrins, Lori
author_sort Buskes, Melissa J.
collection PubMed
description [Image: see text] We recently reported a series of compounds for a solubility-driven optimization campaign of antitrypanosomal compounds. Extending a parasite-hopping approach to the series, a subset of compounds from this library has been cross-screened for activity against the metazoan flatworm parasite, Schistosoma mansoni. This study reports the identification and preliminary development of several potently bioactive compounds against adult schistosomes, one or more of which represent promising leads for further assessment and optimization.
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spelling pubmed-70738862020-03-17 Structure–Bioactivity Relationships of Lapatinib Derived Analogs against Schistosoma mansoni Buskes, Melissa J. Clements, Monica Bachovchin, Kelly A. Jalani, Hitesh B. Leonard, Allison Bag, Seema Klug, Dana M. Singh, Baljinder Campbell, Robert F. Sciotti, Richard J. El-Sakkary, Nelly Caffrey, Conor R. Pollastri, Michael P. Ferrins, Lori ACS Med Chem Lett [Image: see text] We recently reported a series of compounds for a solubility-driven optimization campaign of antitrypanosomal compounds. Extending a parasite-hopping approach to the series, a subset of compounds from this library has been cross-screened for activity against the metazoan flatworm parasite, Schistosoma mansoni. This study reports the identification and preliminary development of several potently bioactive compounds against adult schistosomes, one or more of which represent promising leads for further assessment and optimization. American Chemical Society 2020-01-10 /pmc/articles/PMC7073886/ /pubmed/32184954 http://dx.doi.org/10.1021/acsmedchemlett.9b00455 Text en Copyright © 2020 American Chemical Society This is an open access article published under a Creative Commons Attribution (CC-BY) License (http://pubs.acs.org/page/policy/authorchoice_ccby_termsofuse.html) , which permits unrestricted use, distribution and reproduction in any medium, provided the author and source are cited.
spellingShingle Buskes, Melissa J.
Clements, Monica
Bachovchin, Kelly A.
Jalani, Hitesh B.
Leonard, Allison
Bag, Seema
Klug, Dana M.
Singh, Baljinder
Campbell, Robert F.
Sciotti, Richard J.
El-Sakkary, Nelly
Caffrey, Conor R.
Pollastri, Michael P.
Ferrins, Lori
Structure–Bioactivity Relationships of Lapatinib Derived Analogs against Schistosoma mansoni
title Structure–Bioactivity Relationships of Lapatinib Derived Analogs against Schistosoma mansoni
title_full Structure–Bioactivity Relationships of Lapatinib Derived Analogs against Schistosoma mansoni
title_fullStr Structure–Bioactivity Relationships of Lapatinib Derived Analogs against Schistosoma mansoni
title_full_unstemmed Structure–Bioactivity Relationships of Lapatinib Derived Analogs against Schistosoma mansoni
title_short Structure–Bioactivity Relationships of Lapatinib Derived Analogs against Schistosoma mansoni
title_sort structure–bioactivity relationships of lapatinib derived analogs against schistosoma mansoni
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7073886/
https://www.ncbi.nlm.nih.gov/pubmed/32184954
http://dx.doi.org/10.1021/acsmedchemlett.9b00455
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