Ricerc@Sapienza

Nowadays cancer is one of the most important causes of death. Chemotherapy is the therapeutic strategy that has had the highest evolution in the last years. Nevertheless, a relapse is frequently observed during therapy, due to the development of multidrug resistance. For this reason, it is essential the investigation of a new therapeutic oncological target. The present research project aims to design and synthesize new anticancer drugs targeting ß-catenin. Sulfonamide, ß-catenin inhibitors, combined with NHERF1 inhibitors are expected to inhibit colorectal cancer (CRC). A derivative bearing N-Aryl benzenesulfonamide scaffold inhibit Wnt/ ß-catenin signaling pathway with selective antitumor effect on Wnt-dependent cancer cell in vitro and in mouse models. In this research project, will be carried out a test set of compounds mainly focusing on the substituents at the ring A and the position of the ester functional group at the ring B, to outline the structure-activity relationship in this novel class of ß-catenin inhibitors.