A Bioactive Trypanosoma cruzi Bromodomain Inhibitor from Chemically Engineered Extracts

ACS Combinatorial Science
I Ayelen RamalloRicardo L E Furlan

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.

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Citations

Nov 1, 2018·Chemistry : a European Journal·Haruhisa KikuchiYoshiteru Oshima
Nov 1, 2018·Current Medicinal Chemistry·Victoria Lucia AlonsoEsteban Serra
Nov 19, 2020·ACS Infectious Diseases·Corentine M C LaurinStuart J Conway
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Jul 31, 2019·ACS Combinatorial Science·Carlos M SolísRicardo L E Furlan
Oct 23, 2018·ACS Medicinal Chemistry Letters·Paula GarcíaRicardo L E Furlan
Oct 7, 2021·ACS Infectious Diseases·Cynthia TallantFélix Calderón

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