The present invention relates to a novel compounds for use in treatment or prevention of cancer, in particular to use of said compounds as an inhibitors of interactions between TRF1-TIN2 or TRF2-TIN2 telomeric proteins.

Due to the fact that telomerase is reactivated in most cancerous cells it became a promising target for anticancer chemotherapy. However, despite the fact that telomeres of cancerous cells are usually shorter than telomeres of surrounding cells, decreasing of telomere lengthening by inhibition of telomerase would not cause the immediate cytotoxic effect. Studies in mouse models and in human clinical trials have shown some benefits of telomerase inhibitors (especially Imetelstat) in myeloid malignancies but there are limitations concerning solid tumors. In consequence still there are no clinically approved strategies exploiting this cancer target. As presented studies shows, proposed lead compounds which were obtained by inventors exhibit interesting biological properties, in particular, these compounds interact with the telomeric proteins. This interaction at the molecular level leads to the blocking of the binding of these proteins to the TIN2 protein, which generally disrupts the formation of the shelterin complex. These compounds also show cytotoxicity to neoplastic cells in vitro and ex vivo. It is not a high activity, but it is related to the mechanism of its action as these compounds induce cellular aging in neoplastic cells, which in the long run leads to the death of these cells.

Nencki Institute is the co-owner of the applicable rights with University of Gdańsk, Gdańsk University of Technology, Medical University of Gdańsk, Hirszfeld Institute of Immunology and Experimental Therapy PAS, Pomeranian Hospitals in Gdynia, EU-CONSULT sp. z o.o. and Innovabion sp. z o.o. Gdańsk University of Technology is the leader of patent protection and commercialization related activities.