Synthesis of a novel pentagastrin-drug conjugate for a targeted tumor therapy
2008 | journal article. A publication with affiliation to the University of Göttingen.
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- Authors
- Tietze, Lutz Friedjan; Panknin, Olaf; Major, Felix; Krewer, Birgit
- 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.
- Issue Date
- 2008
- Status
- published
- Publisher
- Wiley-blackwell
- Journal
- Chemistry - A European Journal
- ISSN
- 0947-6539