Abstract: Cantharidin, the active constituent of Mylabris, has displayed significant antitumor activities in vitro and in vivo. The adverse effects on urinary and gastrointestinal tracts prevent it from being accepted by the clinic. In order to search for new antitumor drugs with a high activity and low toxicity, a series of phosphonodipeptide derivatives of exo-bicyclo[2.2.1]heptane (or hept-5-ene )-2, 3-dicarboxylic anhydride were synthesized by the condensation of the corresponding amino acid derivatives of exo-bicyclo[2. 2. 1] hept-5-ene-2, 3-dicarboxylic anhydride with a-aminoalkylphosphonate, and their structures were confrimed by 1H NMR, MSand elemental analysis.

Key words: Cantharidin, exo-Bicyclo[2.2.1]hept-5-ene-2, 3-dicarboxylic anhydride, Phosphonodipeptide