<p>A series of chrysin salicylate derivatives as potential antitumour agents were synthesised and evaluated their antitumour activities <i>in vitro</i> and <i>in vivo</i>. Most of the compounds exhibited moderate to good activities against MCF-7 cells, HepG2 cells, MGC-803cells and MFC cells. Among them, compound <b>3f</b> showed the most potent activity against MGC-803 cells and MFC cells with IC<sub>50</sub> values of 23.83 ± 3.68 and 27.34 ± 5.21 μM, respectively. The flow cytometry assay reconfirmed that compound <b>3f</b> promoted the occurrence of tumour cells’ G1/S block under the inhibiting effect of compound <b>3f</b>. Compound <b>3f</b> possessed higher antitumour efficacy in tumour-bearing mice, compared with the positive control 5-Fu and the blank control saline.</p
