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The intermediates and prodrugs are synthesized with standard organic/peptide chemistry.

 

Peptides are prepared either by solid-phase peptide-syntheis or in solution applying the Fmoc- or Boc-based synthetic methodology. Amide bonds could be obtained form a reaction from a free amino group with a preactivated or in situ activated carboxylic acid. A wide range of coupling reagents can be applied. Introduction of appropriate (orthogonal) protecting groups and their cleavage are necessary steps in some strategies of synthesis.

 

Isolation of the intermediates will generally be performed by FC while the prodrugs by preparative reverse phase HPLC.

 

The purity of the compounds will be identified using analytical HPLC. The compounds will be characterized and their structures will be confirmed by spectral data (MS, NMR, IR).

 

Following the synthesis, in vitro and in vivo studies of the prodrugs will be performed in order to study their cytotoxicity and to assess their efficacy in tumor bearing model.

 

 

 

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