Fungal metabolites based on diketopiperazine scaffolds
Libraries targeting peptides and proteins: For targeting proteins on the cell surface, we focus on natural product scaffolds for various reasons. First, they have been engineered by nature over millions of years for the efficient interaction with biomolecular (mostly protein) receptors. Second, a number of natural products are already known to exhibit a certain degree of specificity for particular types of cancer cells and are thus preevaluated for our purpose. A number of natural products, especially from bacteria, fungi or marine environments, have been a rich source of active compounds in the cancer field. In this context, proline derived diketopiperazines are a class of natural products (mainly fungal metabolites) with a broad biological activity profile.
This thesis involves the development of a new synthetic route to proline derived diketopiperazines and a transfer of the methodology to solid phase chemistry.
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