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. Method: 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. Result: 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.

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喹唑啉-苯并呋喃缀合物的合成和细胞毒活性

目的：研究苯并呋喃的构效关系。背景：苯并呋喃是自然界中广泛存在的一种具有药理作用的天然化合物。新型抗癌苯并呋喃衍生物的开发越来越受到人们的关注。方法：我们将活性喹唑啉单元引入哌嗪取代的苯并呋喃中，制备了一系列喹唑啉苯并呋喃化合物，并通过MTT法评估了对一组人肿瘤细胞系的细胞毒活性。结果：制备了48种新型喹唑啉取代苯并呋喃衍生物，并在体外评价了其对5种人肿瘤细胞系的细胞毒活性。结果表明，一些喹唑啉-苯并呋喃缀合物对肿瘤细胞系表现出选择性抑制活性。结论：