Thirty-one novel genistein amino acid ester derivatives were synthesized and evaluated for their anti-proliferative activities against HUVEC cells and five cancer cells lines (HCT-116, HeLa, HepG-2, MCF-7, MGC-803). Most of the amino acid ester derivatives exhibited more inhibitory activity than their parent compound genistein. In particular, compound 8 j (methyl(4-((5-hydroxy-3-(4-hydroxyphenyl)-4-oxo-4H-chromen-7-yl)oxy)butanoyl)tryptophanate) bearing tryptophan chain showed the most cytotoxicity against HCT-116 cells with IC50 value of 2.76 ...