2-Styrylchromones, a C-2 styrene derivative of chromones, possess a broad spectrum of biological activity. However, 2-styrylchromones are scarce in nature but not to mention the amino-substituted styrylchromones. We have synthesized fourteen 6-amino-2-styrylchromones and evaluated their anti-cancer activity on human caucasian colon adenocarcinoma cells (HT-29). 6-Amino-2-styrylchromones and related derivatives have never been revealed their pharmacology profiles. Among the novel fourteen compounds, we reported that compound 9 h exhibited its potential with the comparable activity with 5-flurouracil (5-FU) as a referenced drug.