Discovery of pyrrole derivatives for the treatment of glioblastoma and chronic myeloid leukemia

Long-term survivors of glioblastoma multiforme (GBM) are at high risk of developing second primary neoplasms, including leukemia. For these patients, the use of classic tyrosine kinase inhibitors (TKIs), such as imatinib mesylate, is strongly discouraged, since this treatment causes a tremendous increase of tumor and stem cell migration and invasion. We aimed to develop agents […]

Targeting beta-catenin and dishevelled protein as a synergistic strategy against colorectal cancer

Research project funded by AIRC. We aim to obtain compounds inhibitors of the Wnt/β-catenin pathway with efficacy for CRC cancer cells. The identified modulators have to be endowed with physicochemical and ADME properties required for drug candidates. The experimental plan is therefore: (1) to test the effect of the different modulators on the Wnt/TCF signaling […]

Sulfonamide inhibitors of beta-catenin signaling with different output on c-MYC as anticancer agents

Laura Di Magno, Fiorella Di Pastena, Michela Puxeddu, Giuseppe La Regina, Antonio Coluccia, Alessia Ciogli, Simone Manetto,Marella Maroder, Gianluca Canettieri, Romano Silvestri, Marianna Nalli. ChemMedChem 2020, 15, 2264-2268. The Wnt/beta-catenin pathway is often found deregulated in cancer. The aberrant accumulation of beta-catenin in the cell nucleus results in the development of various malignancies. Specific drugs against this signaling pathway […]