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Current Organic Synthesis

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ISSN (Print): 1570-1794
ISSN (Online): 1875-6271

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Research Article

Synthesis and Cytotoxic Activity of Quinazoline-benzofuran Conjugates

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

Volume 21, Issue 7, 2024

Published on: 01 August, 2023

Page: [928 - 940] Pages: 13

DOI: 10.2174/1570179420666230623113535

Price: $65

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.

Keywords: Quinazoline, benzofuran, conjugates, synthesis, cytotoxic activity, anticancer.

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