512825-94-4Relevant articles and documents
Pharmacophore-based virtual screening for identification of negative modulators of GLI1 as potential anticancer agents
Manetti, Fabrizio,Stecca, Barbara,Santini, Roberta,Maresca, Luisa,Giannini, Giuseppe,Taddei, Maurizio,Petricci, Elena
supporting information, p. 832 - 838 (2020/10/07)
Starting from known GLI1 inhibitors, a pharmacophore-based virtual screening approach was applied to databases of commercially available compounds with the aim of identifying new GLI1 modulators. As a result, three different chemical scaffolds emerged that were characterized by a significant ability to reduce the transcriptional activity of the endogenous Hedgehog-GLI pathway and GLI1 protein level in murine NIH3T3 cells. They also showed a micromolar antiproliferative activity in human melanoma (A375) and medulloblastoma (DAOY) cell lines, without cytotoxicity in non-neoplastic mammary epithelial cells.