The chemotherapy of malignant tumours is greatly restricted by the
generally slight differentiation of the available cytostatic agents
between normal and malignant tissue. In order to achieve an improvement
of the selectivity in cancer therapy, novel prodrugs have been developed
from 6-hydroxy-2,3-dihydro-1H-indolene,
5-hydroxy-1,2-dihydro-3H-pyrrolo[3,2-e]indolene and
5-hydroxy-1,2-dihydro-3H-benzo[e]indolene as well as from
6-hydroxy-1,2,3,4-tetrahydro-benzo[f]-quinolines, that may be used within
the framework of the ADEP therapy (antibody directed enzyme prodrug
therapy). The new prodrugs are characterised by a high difference in
toxicity between the prodrug and underlying drug and by a very high
efficacy of the drug. After splitting off of the glycosidic and/or acetal
group on the phenolic hydroxy groups of the prodrugs, a
spirocyclopropacyclohexadiene is formed which, being a highly toxic
group, effects an alkylation of the DNA or RNA.