A series of new chromone analogues bearing a substituted arylamine moiety at position-3 were designed and synthesized by a key intermediate 3-iodo-7-methoxy-4H-chromen-4-one (5). All the synthesized compounds exhibited certain antitumor activities against two kinds of human tumor cell lines, colon cancer cell HCT116 and liver cancer cell 7721, in vitro. Five compounds (6c, 6f, 6i, 6m and 6o) were identified as the most promising candidates with the IC50 values in the range of 4.92～12.59 μmol•L－1.

Key words: chromone, buchwald-Hartwig coupling reaction, antitumor activity