【文章名】Synthesis and Biological Studies of Different Duocarmycin Based Glycosidic Prodrugs for Their Use in the Antibody-Directed Enzyme Prodrug Therapy.
[摘要]:The synthesis and biol. evaluation of novel prodrugs for use in the antibody directed enzyme prodrug therapy (ADEPT) of cancer based on the cytotoxic antibiotic duocarmycin SA are described. In this approach, we investigated the influence of the sugar moiety of the glycosidic prodrug on the QIC50 values as well as on the stability and the water soly. The best result was found for prodrug I contg. an a-mannoside moiety with a QIC50 value of 4500.