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Synthesis of a novel pentagastrin-drug conjugate for a targeted tumor therapy.
- Source :
-
Chemistry (Weinheim an der Bergstrasse, Germany) [Chemistry] 2008; Vol. 14 (9), pp. 2811-8. - Publication Year :
- 2008
-
Abstract
- The synthesis of the novel pentagastrin seco-CBI conjugate 3, which is based on the highly cytotoxic antitumor antibiotic (+)-duocarmycin SA (1), is reported. A key step in the synthesis is the palladium-catalyzed carbonylation of aryl bromide 7 to give the benzyl ester 16, which is transformed into the new seco-CBI derivative 21 bearing a carboxylic acid ester moiety. Subsequent transformation of 21 into an activated ester followed by the introduction of beta-alanine and tetragastrin led to the new pentagastrin drug 3 that contains a peptide moiety for targeting cancer cells expressing CCK-B/gastrin receptors.
- Subjects :
- Antineoplastic Agents chemistry
Catalysis
Cell Proliferation drug effects
Drug Delivery Systems
Duocarmycins
Esters chemistry
Molecular Structure
Palladium chemistry
Pentagastrin chemical synthesis
Pyrroles chemistry
Receptor, Cholecystokinin B biosynthesis
Receptor, Cholecystokinin B drug effects
Antineoplastic Agents chemical synthesis
Indoles chemical synthesis
Indoles chemistry
Pentagastrin analogs & derivatives
Pentagastrin chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 0947-6539
- Volume :
- 14
- Issue :
- 9
- Database :
- MEDLINE
- Journal :
- Chemistry (Weinheim an der Bergstrasse, Germany)
- Publication Type :
- Academic Journal
- Accession number :
- 18214880
- Full Text :
- https://doi.org/10.1002/chem.200701521