Chemical modifications of aromatic scaffolds for the development of new G4 ligands

Title: "Chemical modifications of aromatic scaffolds for the development of new G4 ligands" S. Di Ciolo,a S. Galié,a B. Airoldi,a G. Cipolla,a F. Feretti,a C. Giannini,a A. Silvani,a D. Malpicci,a E. Cariati,a E. Lucenti,b D. Montesarchio c aDipartimento di Chimica, Università degli studi di Milano, Milano bCNR-SCITEC, Istituto di Scienze e Tecnologie Chimiche “Giulio Natta”, Milano cDipartimento di Scienze Chimiche, Università di Napoli Federico II, Napoli stefano.diciolo@unimi.it G-quadruplexes (G4s) are non-canonical DNA structures formed by guanine quartets and they are linked to diseases such as cancer.1-2Our group is working on the development of new potential G4-stabilizers. Inspired by recent literature3, we selected three different heterocyclic frameworks potentially capable of binding G4s by stacking onto the external G-tetrads. These scaffolds were functionalized with appropriate polar or positively charged flexible groups to achieve our goal. [1] 10.1016/j.lfs.2024.122481 [2] 10.1016/j.lfs.2024.122481 [3] 10.1002/ejoc.201900692.