Design, Synthesis, and Biological Evaluation of Quinoline (Quinolinone) Derivatives as NADPH Oxidase (NOX) Inhibitors

IF 3.2 4区 医学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY Chemical Biology & Drug Design Pub Date : 2024-08-19 DOI:10.1111/cbdd.14610
Lei Zhang, Xinliang Yang, Rui Yi, Siming Wu, Qianbin Li, Gaoyun Hu, Zhuo Chen
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Abstract

NADPH oxidases (NOXs) are the sole enzyme in the human body that can directly produce reactive oxygen species. Recent studies have shown that NOXs is a very promising target for the treatment of diabetic nephropathy (DN). Here, a series of quinoline(quinolinone) derivatives have been designed based on pharmacophore strategy, synthesized and evaluated. Among them, 19d exhibits potent antiproliferative and NOXs inhibitory activities, and is worthy for further investigation.

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喹啉(喹啉酮)衍生物作为 NADPH 氧化酶(NOX)抑制剂的设计、合成和生物学评价。
NADPH 氧化酶(NOXs)是人体内唯一能直接产生活性氧的酶。最近的研究表明,NOXs 是治疗糖尿病肾病(DN)的一个非常有前景的靶点。本文基于药效学策略设计了一系列喹啉(喹啉酮)衍生物,并对其进行了合成和评价。其中,19d 具有强效的抗增殖和抑制 NOXs 活性,值得进一步研究。
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来源期刊
Chemical Biology & Drug Design
Chemical Biology & Drug Design 医学-生化与分子生物学
CiteScore
5.10
自引率
3.30%
发文量
164
审稿时长
4.4 months
期刊介绍: Chemical Biology & Drug Design is a peer-reviewed scientific journal that is dedicated to the advancement of innovative science, technology and medicine with a focus on the multidisciplinary fields of chemical biology and drug design. It is the aim of Chemical Biology & Drug Design to capture significant research and drug discovery that highlights new concepts, insight and new findings within the scope of chemical biology and drug design.
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