Journal
ACS COMBINATORIAL SCIENCE
Volume 20, Issue 4, Pages 220-228Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acscombsci.7b00172
Keywords
chemically engineered extracts; diversification; bromodomain inhibitor; oxime; Chagas disease
Funding
- FONCYT [PICT2015-3574]
- CONICET [PIP 695]
- Universidad Nacional de Rosario
- [PIP 0685]
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A set of chemically engineered extracts enriched in compounds including N-N and N-O fragments in their structures was prepared. Bromodomain binding screening and bioguided fractionation led to the identification of one oxime hit that interacts with TcBDF3 with affinity in the submicromolar range and that shows interesting antiparasitic properties against the different life cycle stages of T. cruzi.
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