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Structure–Bioactivity Relationships of Lapatinib Derived Analogs against Schistosoma mansoni

Authors :
Lori Ferrins
Melissa J. Buskes
Conor R. Caffrey
Hitesh B. Jalani
Dana M. Klug
Kelly A. Bachovchin
Nelly El-Sakkary
Allison Leonard
Baljinder Singh
Robert F. Campbell
Michael P. Pollastri
Richard J. Sciotti
Seema Bag
Monica Clements
Source :
ACS Medicinal Chemistry Letters
Publication Year :
2020
Publisher :
American Chemical Society, 2020.

Abstract

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.

Details

Language :
English
ISSN :
19485875
Volume :
11
Issue :
3
Database :
OpenAIRE
Journal :
ACS Medicinal Chemistry Letters
Accession number :
edsair.doi.dedup.....dd8ee50ddcb2576fc6178e843d54b7e1