School of Chinese Materia Medica, Yunnan University of Chinese Medicine, Kunming, 650500, P.R. China.
Central Laboratory, The No. 1 Affiliated Hospital of Yunnan University of Chinese Medicine, Kunming, 650021, P.R. China.
Curr Org Synth. 2024;21(7):928-940. doi: 10.2174/1570179420666230623113535.
In order to study on structure-activity relationships of benzofurans.
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.
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.
48 novel quinazoline-substituted benzofuran derivatives have been prepared, and , 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.
We have found that compound 14x displayed excellent cytotoxic activity, which could be considered a potential anticancer agent.
为了研究苯并呋喃的构效关系。
苯并呋喃是一种广泛存在于自然界中的天然化合物，具有多种药理作用。新型抗癌苯并呋喃衍生物的开发越来越受到关注。
我们将一个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-苯并呋喃类化合物，并通过 MTT 法评估了它们对一组人肿瘤细胞系的细胞毒性活性。
合成了 48 种新型喹唑啉取代苯并呋喃衍生物，并评估了它们对 5 个人类肿瘤细胞系的细胞毒性活性。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。
我们发现化合物 14x 表现出优异的细胞毒性活性，可被视为一种有潜力的抗癌药物。
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