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Updated: Jul 25, 2025

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Synthesis and Cytotoxic Activity of Quinazoline-benzofuran Conjugates
Yixin Liu1, Nanting Zou1, Minxin Li1
1School of Chinese Materia Medica, Yunnan University of Chinese Medicine, Kunming, 650500, P.R. China.
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.
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