Structure–Bioactivity Relationships of Lapatinib Derived Analogs against Schistosoma mansoni

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, Schistosom...

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Veröffentlicht in:ACS medicinal chemistry letters 2020-03, Vol.11 (3), p.258-265
Hauptverfasser: 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
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Sprache:eng
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Zusammenfassung: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.
ISSN:1948-5875
1948-5875
DOI:10.1021/acsmedchemlett.9b00455