1 and 2 showed potent cytotoxicity against the human gastric adenocarcinoma (AGS) cell line (IC501; 1.7 and 2; 22.1 nM), as well as strong inhibitory effects against TCF/β-catenin transcription (IC501; 1.8 and 2; 15.9 nM). The gene discussed is HNF4A; the disease is gastric adenocarcinoma.