Glycosidic Prodrugs of Highly Potent Bifunctional Duocarmycin Derivatives for Selective Treatment of Cancer

Cytotoxicities almost a million times lower than the prevailing active compounds, which can have IC50 values of about 100 fM, are displayed by new glycosidic prodrugs for selective tumor therapy (see example; gray C, white H, green Cl, blue N, red O). The cytotoxicity of these new active compounds is presumably not attributable to DNA intra- or DNA inter-strand cross-linking, but might be based on an as yet unknown mechanism.