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

被引：1
|
作者：
Ramos-Soriano, Javier [1 ,3 ]
Holbrow-Wilshaw, Maisie [1 ]
Hunt, Eliza [1 ]
Jiang, Y. Jennifer [1 ]
Penalver, Pablo [2 ]
Morales, Juan C. [2 ]
Galan, M. Carmen [1 ]
机构：
[1] Univ Bristol, Sch Chem, Bristol BS8 1TS, England
[2] CSIC, PTS Granada, Inst Parasitol & Biomed Lopez Neyra, Ave Conocimiento 17, Armilla 18016, Granada, Spain
[3] Univ Seville, Inst Invest Quim IIQ, CSIC, Ave Amer Vespucio 49, Seville 41092, Spain
来源：
CHEMICAL COMMUNICATIONS | 2024年 / 60卷 / 81期
基金：
英国工程与自然科学研究理事会;
关键词：
TELOMERIC DNA; IDENTIFICATION;
D O I：
10.1039/d4cc03106g
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
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. Azobenzene ligands targeting G4 DNA exhibit subnanomolar antiparasitic activity against T. brucei and a remarkable selectivity index (IC50 MRC-5/T. brucei) of 2285-fold.
引用
收藏
页码：11520 / 11523
页数：4
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