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MDPI, Molecules, 3(24), p. 426, 2019

DOI: 10.3390/molecules24030426



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Naphthalene Diimides as Multimodal G-Quadruplex-Selective Ligands

Journal article published in 2019 by Valentina Pirota ORCID, Matteo Nadai, Filippo Doria, Sara Richter
This paper is made freely available by the publisher.
This paper is made freely available by the publisher.

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G-quadruplexes are four-stranded nucleic acids structures that can form in guanine-rich sequences. Following the observation that G-quadruplexes are particularly abundant in genomic regions related to cancer, such as telomeres and oncogenes promoters, several G-quadruplex-binding molecules have been developed for therapeutic purposes. Among them, naphthalene diimide derivatives have reported versatility, consistent selectivity and high affinity toward the G-quadruplex structures. In this review, we present the chemical features, synthesis and peculiar optoelectronic properties (absorption, emission, redox) that make naphtalene diimides so versatile for biomedical applications. We present the latest developments on naphthalene diimides as G-quadruplex ligands, focusing on their ability to bind G-quadruplexes at telomeres and oncogene promoters with consequent anticancer activity. Their different binding modes (reversible versus irreversible/covalent) towards G-quadruplexes and their additional use as antimicrobial agents are also presented and discussed.