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Synthesis and Biological Studies of Different Duocarmycin Based Glycosidic Prodrugs for Their Use in the Antibody-Directed Enzyme Prodrug Therapy

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journal contribution
posted on 22.01.2009 by Lutz F. Tietze, Heiko J. Schuster, Birgit Krewer, Ingrid Schuberth
The synthesis and biological evaluation of novel prodrugs for use in the antibody directed enzyme prodrug therapy (ADEPT) of cancer based on the cytotoxic antibiotic duocarmycin SA (1) 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 solubility. The best result was found for prodrug 22 containing an α-mannoside moiety with a QIC50 value of 4500.

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