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A Bioactive Trypanosoma cruzi Bromodomain Inhibitor from Chemically Engineered Extracts
ACS Combinatorial Science ( IF 3.903 ) Pub Date : 2018-02-26 00:00:00 , DOI: 10.1021/acscombsci.7b00172
I. Ayelen Ramallo 1, 2 , Victoria L. Alonso 1, 2 , Federico Rua 2 , Esteban Serra 1, 3 , Ricardo L. E. Furlan 1, 2
Affiliation  

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.

中文翻译:

化学工程提取物中的一种生物活性克氏锥虫溴结构域抑制剂。

制备了一组化学工程提取物,这些提取物的结构中富含N–N和N–O片段。溴基结构域结合的筛选和bioguided分馏导致酮肟命中识别与相互作用BDF3并与在亚微摩尔范围亲和力显示了对不同的生命周期阶段有趣抗寄生虫药物锥虫
更新日期:2018-02-26
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