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Naphthalene diimide-naphthalimide dyads promote telomere damage by selectively targeting multimeric G-quadruplexes.


ABSTRACT: G-quadruplex (G4) nucleic acid ligands have attracted significant attention as putative anticancer agents for selectively stabilizing telomeric structures. In our pursuit of targeting the most biologically relevant telomeric structures, we have investigated a new class of naphthalene diimide (NDI)-based ligands designed to bind multimeric G4s. The NDI unit covalently linked with one 1,8-naphthalimide (NI) moiety, results in ligands able to fold into a sandwich-like conformation fitting into the binding pockets of telomeric multimeric G4s, thus optimizing binding complementarity. Varying the NDI decorations, we synthesized a small library of NDI-NI dyads and then examined their capability of stabilizing G4s by biophysical assays. Given the relevance of G4 stabilizing agents in fighting canc

SUBMITTER: Pirota V 

PROVIDER: S-EPMC12000870 | biostudies-literature | 2025 Apr

REPOSITORIES: biostudies-literature