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Current Organic Synthesis

Author(s): Yixin Liu, Nanting Zou, Minxin Li, Chunping Wan* and Zewei Mao*

DOI: 10.2174/1570179420666230623113535

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Synthesis and Cytotoxic Activity of Quinazoline-benzofuran Conjugates

Page: [928 - 940] Pages: 13

  • * (Excluding Mailing and Handling)

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.

Graphical Abstract

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