<p>Two new 2-arylbenzofuran derivatives, moracinfurol A and B (<b>1</b>–<b>2</b>), and ten known compounds (<b>3</b>–<b>12</b>) were isolated from the leaves of <i>Morus alba.</i> Their structures were determined on the basis of spectroscopic analysis including 1D, 2D NMR and HR-ESI-MS. All of the 2-arylbenzofuran derivatives were evaluated for cytotoxicity against A549 cells. Some cytotoxic 2-arylbenzofuran derivatives might induce autophagy characterized by the accumulation of LC-3 Ⅱ.</p