AbstractThirty‐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 cel...