A STUDY ON ANTITUMOR CHEMOTHERAPEUTIC AGENTS——SYNTHESIS OF N-CANTHARIDINE DERIVATIVES

Cantharidine is known to have efficacy for the treatment of cancer. The adverse effects on urinary and gastrointestinal tracts prevent it to be accepted by the clinic. The structural modification of cantharidine is pursued by the author with the aim to decrease its toxicity and increase its efficacy.Fifteen novel N-derivatives of cantharidine were synthesized. Compound Ⅺ brought about 40% inhibitory action on tumour S-180 in animals. It may be a potential antitumor drug. Some of the derivatives were shown to have certain inhibitory action on tumout, S-180 and EAC, The derivatives prepared are listed in table 1.