Design, synthesis and biological evaluation of chrysin benzimidazole derivatives as potential anticancer agents

<p>A series of chrysin benzimidazole derivatives were synthesised and evaluated for their anticancer activity in the search for potential anticancer agents. Among them, compound <b>18</b> displayed the most potent anti-proliferative activity against MFC cells with IC₅₀ values of 25.72 ± 3.95 μM. The flow cytometry results displayed that compound <b>18</b> induced apoptosis of MFC cells in a dose-dependent manner and caused the cell cycle to be arrested in the G0/G1 phase. Furthermore, the preliminary anticancer activity <i>in vivo</i> was also studied in tumour-bearing mice, and the compound <b>18</b> exerted good inhibition effect on tumour growth. These results suggested that compound <b>18</b> had good anticancer activity, which could be a potential anticancer agent after further optimisation and evaluation.</p

Synthesis and evaluation of antitumour activity <i>in vitro</i> and <i>in vivo</i> of chrysin salicylate derivatives

<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 IC₅₀ 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