Synthesis and Cytotoxic Activity of Quinazoline-benzofuran Conjugates.

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.