Yixin Liu, Nanting Zou, Minxin Li, Chunping Wan, Zewei Mao
{"title":"Synthesis and Cytotoxic Activity of Quinazoline-benzofuran Conjugates.","authors":"Yixin Liu, Nanting Zou, Minxin Li, Chunping Wan, Zewei Mao","doi":"10.2174/1570179420666230623113535","DOIUrl":null,"url":null,"abstract":"<p><strong>Aims: </strong>In order to study on structure-activity relationships of benzofurans.</p><p><strong>Background: </strong>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.</p><p><strong>Methods: </strong>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.</p><p><strong>Results: </strong>48 novel quinazoline-substituted benzofuran derivatives have been prepared, and <i>in vitro</i>, 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.</p><p><strong>Conclusion: </strong>We have found that compound 14x displayed excellent cytotoxic activity, which could be considered a potential anticancer agent.</p>","PeriodicalId":11101,"journal":{"name":"Current organic synthesis","volume":null,"pages":null},"PeriodicalIF":1.7000,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Current organic synthesis","FirstCategoryId":"92","ListUrlMain":"https://doi.org/10.2174/1570179420666230623113535","RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, ORGANIC","Score":null,"Total":0}
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.
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.