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Glycosidic Prodrugs of Highly Potent Bifunctional Duocarmycin Derivatives for Selective Treatment of Cancer
Author(s) -
Tietze Lutz F.,
von Hof J. Marian,
Müller Michael,
Krewer Birgit,
Schuberth Ingrid
Publication year - 2010
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201002502
Subject(s) - prodrug , glycosidic bond , chemistry , bifunctional , stereochemistry , diastereomer , combinatorial chemistry , biochemistry , enzyme , catalysis
Cytotoxicities almost a million times lower than the prevailing active compounds, which can have IC 50 values of about 100 f M , 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.