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. 2018 Apr 9;20(4):220-228.
doi: 10.1021/acscombsci.7b00172. Epub 2018 Mar 2.

A Bioactive Trypanosoma cruzi Bromodomain Inhibitor from Chemically Engineered Extracts

I Ayelen Ramallo  1   2 , Victoria L Alonso  1   2 , Federico Rua  2 , Esteban Serra  1   3 , Ricardo L E Furlan  1   2
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A Bioactive Trypanosoma cruzi Bromodomain Inhibitor from Chemically Engineered Extracts

I Ayelen Ramallo et al. ACS Comb Sci. .

Abstract

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.

Keywords: Chagas disease; bromodomain inhibitor; chemically engineered extracts; diversification; oxime.

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