During recent studies on development new inhibitor of thioredoxin system inhibitors, the new class of β-acyloxyamides I has been found. Studied peptidomimetics exhibited interesting biological properties and were very potent anticancer agents either in vitro (in cellular assays) or in vivo (mice model). [1,2]

Detailed mechanistic studies indicated, however, that compound I activates apoptotic pathways not only by inhibiting the thioredoxin system. To establish mechanism of action of new compounds in a cell, we developed marker compounds containing fluorescent fragments as well as biotinylated compounds 1 and 2. Here, we will present the proposed methodology as well as the results of studies on the synthesis of compounds 1 and 2.

[1]: Klossowski, S., Muchowicz, A., Firczuk, M., Swiech, M., Redzej, A., Golab, J., Ostaszewski, R., J. Med. Chem. 2012, 55, 1, p. 55 - 67

[2]: Ostaszewski, R., Klossowski, S., Szokalska, A., Swiech, M., Ziuzia I., Golab, J., Patent App. PK/1081/AG

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2. Studies toward Novel Peptidomimetc Inhibitors of Thioredoxin-Thiredoxin Reductase System
3. Synthesis and biological evaluation of new inhibitors of thioredoxin - thioredoxin reductase.
4. Chemoenzymatic approach to the synthesis of bioactive tripeptide mimetics for treatment of cancer
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