Synthesis of α-aminoalkyl phosphonate derivatives of resveratrol as potential antitumour agents

Several alpha-aminoalkyl phosphonate derivatives of resveratrol were first prepared by partial synthesis from resveratrol. Antitumour activities of the synthesized compounds were determined against a human nasopharyngeal epidermoid tumour cell line KB and a human normal cell line L02 in vitro. The results indicated that these compounds showed good cytotoxic activity against KB but weak cytotoxic activity against L02. Compounds 5c and 5d showed significant cytotoxic activity against KB, with median inhibition concentration (IC50) values of 0.4 mu M and 0.9 mu M, respectively. On the basis of the biological results, the structure-activity relationship is discussed concisely. The potent antitumour activities shown by 5c and 5d make these resveratrol phosphonate derivatives of great interest for further investigations.