Probing the binding and antiparasitic efficacy of azobenzene G-quadruplex ligands to investigate G4 ligand design†

IF 4.3 2区化学 Q2 CHEMISTRY, MULTIDISCIPLINARY

Chemical Communications Pub Date : 2024-09-13 DOI:10.1039/d4cc03106g

引用次数: 0

Abstract

Novel strategies against parasitic infections are of great importance. Here, we describe a G4 DNA ligand with subnanomolar antiparasitic activity against T. brucei and a remarkable selectivity index (IC₅₀ MRC-5/T. brucei) of 2285-fold. We also correlate the impact of small structural changes to G4 binding activity and antiparasitic activity.

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探究偶氮苯 G-四链配体的结合和抗寄生虫功效，研究 G4 配体的设计原则

针对寄生虫感染的新策略非常重要。在这里，我们描述了一种 G4 DNA 配体，它对布氏杆菌具有亚纳摩尔抗寄生虫活性，选择性指数（IC50 MRC-5/T.brucei）高达 2285 倍。我们还研究了微小结构变化对 G4 结合活性和抗寄生虫活性的影响。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Chemical Communications 化学-化学综合

CiteScore

8.60

自引率

4.10%

发文量

2705

审稿时长

1.4 months

期刊介绍： ChemComm (Chemical Communications) is renowned as the fastest publisher of articles providing information on new avenues of research, drawn from all the world''s major areas of chemical research.