Naoto Kojima, Tetsuya Fushimi, Takahiro Tatsukawa, Tetsuaki Tanaka, Mutsumi Okamura, Akinobu Akatsuka, Takao Yamori, Shingo Dan, Hiroki Iwasaki, Masayuki Yamashita
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.
October 30, 2014: European Journal of Medicinal Chemistry