227084-60-8Relevant academic research and scientific papers
Synthesis of fluorescence-labelled glycosidic prodrugs based on the cytotoxic antibiotic duocarmycin
Tietze, Lutz F.,Behrendt, Frank,Major, Felix,Krewer, Birgit,Von Hof, J. Marian
experimental part, p. 6909 - 6921 (2011/02/23)
The synthesis of the glycosidic prodrugs (1S)-30a, (1S,10R)-30b and (1S,10R)-32 labelled with different fluorescence dyes at different positions at the aromatic A-ring in 2 is described; the compounds are structurally based on the cytotoxic antibiotic duocarmycin SA. For binding, the amino compounds (1S)-3a and (1S,10R)-3b were treated with the commercially available succinimides of the dyes 5-SFX (29) and D10162 (31), respectively. Fluorescence-labelled compounds can be used for verification of interaction with cellular targets on the molecular level by use of confocal laser scanning microscopy for cell cultures and the Explore-Optics instrument (GE) for mice. The described fluorescence-labelled glycosidic prodrugs based on the cytotoxic antibiotic duocarmycine SA have high potential for selective treatment of cancer. Copyright
