Abstract: Six 2′,6′-dihydroxy-substituted-chalcones (Ⅳa—f), twenty 2′-hydroxy-substituted chalcones (Ⅴa—t) and six substituted chalcones (Ⅵa—f) were prepared as potential antitumour agents. Preliminary biological test indicated that compounds Ⅳd, Ⅴa, Ⅴb, Ⅴc, Ⅴe, Ⅴf and Ⅴi possessed inhibitory action in vitro against Ehrlich ascites tumour at a concentration of 125γ/ml, and compounds Ⅳa, Ⅳb, Ⅳf, Ⅴd, Ⅴk, Ⅴr, Ⅴs, Ⅵa, Ⅵb, Ⅵc and Ⅵf also showed inhibiting action against the same turnout at a concentration of 250γ/ml in vitro. However, none of them showed any significant activity against Ehrlich ascites tumour or sarcoma-180 in mice.