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Synthesis and biological studies of different duocarmycin based glycosidic prodrugs for their use in the antibody-directed enzyme prodrug therapy.
- Source :
-
Journal of medicinal chemistry [J Med Chem] 2009 Jan 22; Vol. 52 (2), pp. 537-43. - Publication Year :
- 2009
-
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.
- Subjects :
- Chromatography, High Pressure Liquid
Duocarmycins
Indoles chemistry
Magnetic Resonance Spectroscopy
Neoplasms drug therapy
Prodrugs chemistry
Pyrroles chemical synthesis
Pyrroles chemistry
Pyrroles pharmacology
Spectrometry, Mass, Electrospray Ionization
Antibodies therapeutic use
Glycosides chemistry
Indoles chemical synthesis
Indoles pharmacology
Neoplasms therapy
Prodrugs chemical synthesis
Prodrugs pharmacology
beta-Galactosidase therapeutic use
Subjects
Details
- Language :
- English
- ISSN :
- 1520-4804
- Volume :
- 52
- Issue :
- 2
- Database :
- MEDLINE
- Journal :
- Journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 19143570
- Full Text :
- https://doi.org/10.1021/jm8009102