An overview of quadruplex ligands: Their common features and chemotype diversity

Pirota, Valentina; Stasi, Michele; Benassi, Alessandra; Doria, Filippo

doi:10.1016/bs.armc.2020.04.008

Cited by 16 publications

(19 citation statements)

References 109 publications

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“…Thus, these studies indicate that chemical modifications of TO are needed to provide TO-based probes with selectivity toward G-quadruplexes ( Figure 7 b). The interest in selectively targeting G-quadruplexes has resulted in the discovery of many molecular ligands which exhibit high affinity towards G-quadruplexes [ 112 ]. Most commonly, such ligands consist of flat aromatic structures that can form stacking interactions with the planar G-quadruplexes.…”

Section: Sensing Of Nucleic Acidsmentioning

confidence: 99%

Broad Applications of Thiazole Orange in Fluorescent Sensing of Biomolecules and Ions

Suss,

Motiei,

Margulies

2021

Molecules

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Fluorescent sensing of biomolecules has served as a revolutionary tool for studying and better understanding various biological systems. Therefore, it has become increasingly important to identify fluorescent building blocks that can be easily converted into sensing probes, which can detect specific targets with increasing sensitivity and accuracy. Over the past 30 years, thiazole orange (TO) has garnered great attention due to its low fluorescence background signal and remarkable ‘turn-on’ fluorescence response, being controlled only by its intramolecular torsional movement. These features have led to the development of numerous molecular probes that apply TO in order to sense a variety of biomolecules and metal ions. Here, we highlight the tremendous progress made in the field of TO-based sensors and demonstrate the different strategies that have enabled TO to evolve into a versatile dye for monitoring a collection of biomolecules.

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Section: Sensing Of Nucleic Acidsmentioning

confidence: 99%

Broad Applications of Thiazole Orange in Fluorescent Sensing of Biomolecules and Ions

Suss,

Motiei,

Margulies

2021

Molecules

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“…In this context, Freccero’s group published, in 2012, the synthesis and the biophysical studies of a family of polyheterocyclic 1,2,4-oxadiazoles ligands ( BOxAzaPys , Figure 9 ) [ 81 ]. These ligands, mimicking the well-known macrocyclic G4 binder telomestatin [ 82 ], were able to selectively interact and stabilize telomeric G4, inhibiting the activity of telomerase. This new family of acyclic G4 ligands was characterized by excellent water solubility and an unexpected potential.…”

Section: Nucleic Acid Structures As Oxadiazole Targetsmentioning

confidence: 99%

Groundbreaking Anticancer Activity of Highly Diversified Oxadiazole Scaffolds

Benassi

Doria

Pirota

2020

IJMS

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Nowadays, an increasing number of heterocyclic-based drugs found application in medicinal chemistry and, in particular, as anticancer agents. In this context, oxadiazoles—five-membered aromatic rings—emerged for their interesting biological properties. Modification of oxadiazole scaffolds represents a valid strategy to increase their anticancer activity, especially on 1,2,4 and 1,3,4 regioisomers. In the last years, an increasing number of oxadiazole derivatives, with remarkable cytotoxicity for several tumor lines, were identified. Structural modifications, that ensure higher cytotoxicity towards malignant cells, represent a solid starting point in the development of novel oxadiazole-based drugs. To increase the specificity of this strategy, outstanding oxadiazole scaffolds have been designed to selectively interact with biological targets, including enzymes, globular proteins, and nucleic acids, showing more promising antitumor effects. In the present work, we aim to provide a comprehensive overview of the anticancer activity of these heterocycles, describing their effect on different targets and highlighting how their structural versatility has been exploited to modulate their biological properties.

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“…In this context, Freccero's group published, in 2012, the synthesis and the biophysical studies of a family of polyheterocyclic 1,2,4-oxadiazoles ligands (BOxAzaPys, Figure 9) [81]. These ligands, mimicking the well-known macrocyclic G4 binders Telomestatin [82], were able to selectively interact and stabilize telomeric G4, inhibiting the activity of telomerase. This new family of acyclic G4 ligands was characterized by excellent water solubility and an unexpected potential.…”

Section: Nucleic Acid Structures As Oxadiazole Targetsmentioning

confidence: 99%

Groundbreaking Anticancer Activity of Highly Diversified Oxadiazole Scaffolds

Benassi

Doria

Pirota

2020

Preprint

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Nowadays, an increasing number of heterocyclic-based drugs found application in medicinal chemistry and, in particular, as anticancer agents. In this context, oxadiazoles, five-membered aromatic rings, emerged for their interesting biological properties. Modification of oxadiazole scaffolds represents a valid strategy to increase their anticancer activity, especially on 1,2,4 and 1,3,4 regioisomers. In the last years, an increasing number of oxadiazole derivatives, with remarkable cytotoxicity for several tumor lines, were identified. Structural modifications, that ensure higher cytotoxicity towards malignant cells, represent a solid starting point in the development of novel oxadiazoles-based drugs. To increase the specificity of this strategy, outstanding oxadiazole scaffolds have been designed to selectively interact with biological targets, including enzymes, globular proteins and nucleic acids, showing more promising antitumor effects. In the present work, we aim to provide a comprehensive overview of the anticancer activity of these heterocycles, describing their effect on different targets and highlighting how their structural versatility has been exploited to modulate their biological properties.

show abstract

An overview of quadruplex ligands: Their common features and chemotype diversity

Cited by 16 publications

References 109 publications

Broad Applications of Thiazole Orange in Fluorescent Sensing of Biomolecules and Ions

Broad Applications of Thiazole Orange in Fluorescent Sensing of Biomolecules and Ions

Groundbreaking Anticancer Activity of Highly Diversified Oxadiazole Scaffolds

Groundbreaking Anticancer Activity of Highly Diversified Oxadiazole Scaffolds

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