Development of 3-methyl/3-(morpholinomethyl)benzofuran derivatives as novel antitumor agents towards non-small cell lung cancer cells.

As one of the most lethal malignancies, lung cancer is considered to account for approximately one-fifth of all malignant tumours-related deaths worldwide. This study reports the synthesis and biological assessment of two sets of 3-methylbenzofurans (, , and ) and 3-(morpholinomethyl)benzofurans (, , and ) as potential anticancer agents towards non-small cell lung carcinoma A549 and NCI-H23 cell lines, with VEGFR-2 inhibitory activity. The target benzofuran-based derivatives efficiently inhibited the growth of both A549 and NCI-H23 cell lines with IC spanning in ranges 1.48-47.02 and 0.49-68.9 µM, respectively. The three most active benzofurans (, and ) were further investigated for their effects on the cell cycle progression and apoptosis in A549 (for ) and NCI-H23 (for and ) cell lines. Furthermore, benzofurans , and displayed good VEGFR-2 inhibitory activity with IC equal 77.97, 132.5 and 45.4 nM, respectively.