Synthesis and biological studies of different duocarmycin based glycosidic prodrugs for their use in the antibody-directed enzyme prodrug therapy.

Abstract:

: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 QIC(50) values as well as on the stability and the water solubility. The best result was found for prodrug 22 containing an alpha-mannoside moiety with a QIC(50) value of 4500.

journal_name

J Med Chem

authors

Tietze LF,Schuster HJ,Krewer B,Schuberth I

doi

10.1021/jm8009102

subject

Has Abstract

pub_date

2009-01-22 00:00:00

pages

537-43

issue

2

eissn

0022-2623

issn

1520-4804

pii

10.1021/jm8009102

journal_volume

52

pub_type

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