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| Content Provider | World Health Organization (WHO)-Global Index Medicus |
|---|---|
| Author | Schmuck, Kianga Schuster, Heiko J. Müller, Michael Tietze, Lutz F. Schuberth, Ingrid |
| Description | Author Affiliation: Tietze LF ( Institut für Organische und Biomolekulare Chemie, Georg-August-Universität Göttingen, Tammannstraße 2, 37077 Göttingen, Germany. ltietze@gwdg.de) |
| Abstract | 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. |
| ISSN | 09476539 |
| e-ISSN | 15213765 |
| Journal | Chemistry - A European Journal |
| Issue Number | 6 |
| Volume Number | 17 |
| Language | English |
| Publisher | Wiley-VCH;ChemPubSoc Europe |
| Publisher Date | 2011-02-07 |
| Publisher Place | Germany |
| Access Restriction | Open |
| Subject Keyword | DNA Metabolism Drug Design Indoles Prodrugs Antibodies Therapeutic Use Drug Screening Assays, Antitumor Glucuronidase Chemical Synthesis Chemistry Inhibitory Concentration 50 Molecular Structure Pyrroles Research Support, Non-U.S. Gov't |
| Content Type | Text |
| Resource Type | Article |
| Subject | Organic Chemistry Catalysis |
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