Thiophene-3-carboxamide analogue of annonaceous acetogenins as antitumor drug lead.
Kojima N, Fushimi T, Tatsukawa T, Tanaka T, Okamura M, Akatsuka A, Yamori T, Dan S, Iwasaki H, Yamashita M.
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.