Synthesis and Cytotoxic Activity of Quinazoline-benzofuran Conjugates.

IF 1.7 4区 化学 Q3 CHEMISTRY, ORGANIC
Yixin Liu, Nanting Zou, Minxin Li, Chunping Wan, Zewei Mao
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引用次数: 0

Abstract

Aims: In order to study on structure-activity relationships of benzofurans.

Background: Benzofuran is a kind of natural compound widely existing in nature with pharmacological effects. The development of new anticancer benzofuran derivatives has attracted more and more attention.

Methods: We have introduced an active quinazoline unit into piperazine-substituted benzofuran, prepared a series of quinazoline-benzofuran compounds, and evaluated cytotoxic activity against a panel of human tumor cell lines by MTT assay.

Results: 48 novel quinazoline-substituted benzofuran derivatives have been prepared, and in vitro, cytotoxic activity against five human tumor cell lines was evaluated. The results indicated that some quinazoline-benzofuran conjugates showed selective inhibitory activity against tumor cell lines.

Conclusion: We have found that compound 14x displayed excellent cytotoxic activity, which could be considered a potential anticancer agent.

喹唑啉-苯并呋喃共轭物的合成与细胞毒性活性
目的:研究苯并呋喃类化合物的结构-活性关系:背景:苯并呋喃是一种广泛存在于自然界并具有药理作用的天然化合物。背景:苯并呋喃是一种广泛存在于自然界并具有药理作用的天然化合物,开发新的抗癌苯并呋喃衍生物已引起越来越多的关注:方法:我们在哌嗪取代的苯并呋喃中引入了活性喹唑啉单元,制备了一系列喹唑啉-苯并呋喃化合物,并通过 MTT 试验评估了这些化合物对人类肿瘤细胞株的细胞毒活性:结果:制备了48种新型喹唑啉取代苯并呋喃衍生物,并在体外评估了它们对5种人类肿瘤细胞株的细胞毒活性。结果表明,一些喹唑啉-苯并呋喃共轭物对肿瘤细胞株具有选择性抑制活性:结论:我们发现化合物 14x 具有很好的细胞毒活性,可视为一种潜在的抗癌剂。
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来源期刊
Current organic synthesis
Current organic synthesis 化学-有机化学
CiteScore
3.40
自引率
5.60%
发文量
86
审稿时长
6-12 weeks
期刊介绍: Current Organic Synthesis publishes in-depth reviews, original research articles and letter/short communications on all areas of synthetic organic chemistry i.e. asymmetric synthesis, organometallic chemistry, novel synthetic approaches to complex organic molecules, carbohydrates, polymers, protein chemistry, DNA chemistry, supramolecular chemistry, molecular recognition and new synthetic methods in organic chemistry. The frontier reviews provide the current state of knowledge in these fields and are written by experts who are internationally known for their eminent research contributions. The journal is essential reading to all synthetic organic chemists. Current Organic Synthesis should prove to be of great interest to synthetic chemists in academia and industry who wish to keep abreast with recent developments in key fields of organic synthesis.
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