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

Abstract

<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