<jats:title>Abstract</jats:title><jats:p>Nineteen compounds have been isolated from the methanol extract of the root and aerial parts <jats:italic>of Ruta graveolens</jats:italic>. The structural elucidation of these isolated compounds were determined by the spectroscopic methods and/or comparison of the physical data with literature values. Their antiplatelet aggregation and cytotoxic activities were examined to find potent antiplatelet aggregation and cytotoxic compounds from natural resources. Among them, dictamine (<jats:bold>5</jats:bold>), skimmianine (<jats:bold>7</jats:bold>), psoralen (<jats:bold>8</jats:bold>), chalepensin (<jats:bold>12</jats:bold>), clausindin (<jats:bold>13</jats:bold>), and graveolinine (<jats:bold>16</jats:bold>) showed significant inhibition of platelet aggregation, induced by arachidonic acid and collagen. Arborinine (<jats:bold>2</jats:bold>), dictamine (<jats:bold>5</jats:bold>), isopimpinellin (<jats:bold>11</jats:bold>), clausindin (<jats:bold>13</jats:bold>), and graveoline (<jats:bold>17</jats:bold>) exhibited cytotoxic activity against KB, Hela, DLD, NCI and Hepa tumor cell lines.