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.