Synthesis, characterisation and evaluation of anticancer activity of 1,8-naphthimide derivatives

In this paper, two novel naphthalimide derivatives, D-1 and D-2 as potential antitumour agents. The molecular docking of the two compounds with DNA-Topo II and dsDNA was simulated using MOE. And it was hypothesised that the compounds bind to DNA in the mode of insertion. D-1 and D-2 could be inserted into the base pairs of DNA, respectively, resulting in a conformational change of DNA. The antiproliferative activities of D-1 and D-2 against lung cancer cells A549 were evaluated by MTT method with IC50 values of 14.37 μg mL-1 and 20.12 μg mL-1, respectively. And it was found that the inhibitory effects of these two compounds were stronger than those of the positive drugs, amonafide (63.61 μg mL-1) and mitonafide (55.36 μg mL-1).