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Synthesis and Biological Evaluation of Prodrugs Based on the Natural Antibiotic Duocarmycin for Use in ADEPT and PMT
Author(s) -
Tietze Lutz F.,
Schmuck Kianga,
Schuster Heiko J.,
Müller Michael,
Schuberth Ingrid
Publication year - 2011
Publication title -
chemistry – a european journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.687
H-Index - 242
eISSN - 1521-3765
pISSN - 0947-6539
DOI - 10.1002/chem.201002798
Subject(s) - prodrug , adept , pharmacology , chemistry , antibiotics , medicine , combinatorial chemistry , computational biology , biochemistry , biology
Chemotherapy of malign tumors is usually associated with serious side effects as common anticancer drugs lack selectivity. An approach to deal with this problem is the antibody‐directed enzyme prodrug therapy (ADEPT) and the prodrug monotherapy (PMT). Herein, the synthesis and biological evaluation of new glycosidic prodrugs suitable for both concepts are described. All prodrugs but one are stable in human serum and show QIC 50 values (IC 50 of prodrug/IC 50 of prodrug in the presence of the appropriate glycohydrolase) of up to 6500. This is the best value found so far for compounds interacting with DNA.