Thiophene-3-carboxamide analogue of annonaceous acetogenins as antitumor drug lead

• Five heterocyclic analogues of annonaceous acetogenins were synthesized.
• The analogues showed growth inhibitory activity toward human cancer cell lines.
• Thiophene-2-carboxamide analogue inhibited NCI-H23 growth in xenograft mouse assay.

Five novel acetogenin analogues with a furan, thiophene, or thiazole ring were synthesized, and their inhibitory activities toward human cancer cell lines were evaluated. The analogues showed more potent activities than natural acetogenin. One of them, the thiophene-3-carboxamide analogue, strongly inhibited the growth of human lung cancer cell line NCI-H23 in the xenograft mouse assay without critical toxicity.

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