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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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Detalles Bibliográficos
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
Descripción
Sumario:[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.