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Related Experiment Video

Updated: Sep 17, 2025

Author Spotlight: Characterizing DNA G-Quadruplex by Bis-3-Chloropiperidine Based Chemical Mapping
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Combining Cyclic Triimidazo Triazine Core With Ethynyl-N-Methyl-Pyridinium Groups for Targeting G-Quadruplex

Chiara Platella1, Stefano Di Ciolo2, Andrea Criscuolo1

  • 1Department of Chemical Sciences, University of Naples Federico II, Napoli, Italy.

Archiv Der Pharmazie
|July 3, 2025
PubMed
Summary

New cyclic triimidazo triazine (TT) derivatives target cancer-related DNA G-quadruplex structures. These compounds show specific binding and stabilization, with an alkyne linker enhancing anticancer activity.

Keywords:
G‐quadruplex ligandsantiproliferative activitybiophysical characterizationchemical synthesiscyclic triimidazo triazine derivatives

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Area of Science:

  • Medicinal Chemistry
  • Chemical Biology
  • Biochemistry

Background:

  • DNA G-quadruplexes are promising anticancer targets due to their role in telomere maintenance and oncogene regulation.
  • Developing small molecules that selectively bind and modulate G-quadruplex structures is a key strategy in cancer therapy.

Purpose of the Study:

  • To synthesize and characterize a mini-library of cyclic triimidazo triazine (TT) derivatives functionalized with ethynyl-N-methyl-pyridinium moieties.
  • To evaluate the G-quadruplex binding affinity, selectivity, and stabilizing properties of these novel compounds.
  • To investigate the structure-activity relationships, including the role of the alkyne linker and substitution patterns.

Main Methods:

  • Synthesis and characterization of TT derivatives.
  • Affinity chromatography, spectroscopic, and electrophoretic techniques for G-quadruplex binding assays.
  • Molecular docking simulations to elucidate binding modes.
  • Biological assays to assess anticancer activity.

Main Results:

  • The synthesized TT derivatives effectively recognized and bound to G-quadruplex structures from telomeric and oncogene promoter sequences.
  • The TT core interacted with outer G-quartets, while N-methyl-pyridinium groups engaged with G-quadruplex grooves.
  • Trisubstituted derivatives exhibited stronger stabilization than di- and monosubstituted analogs, but lower selectivity over duplex DNA.
  • The presence of an alkyne linker significantly enhanced G-quadruplex stabilization and anticancer activity.

Conclusions:

  • Cyclic triimidazo triazine derivatives are effective G-quadruplex binders and stabilizers.
  • The substitution pattern influences binding affinity, selectivity, and stabilizing effects.
  • The alkyne linker is crucial for optimizing G-quadruplex interaction and enhancing anticancer potential, highlighting its therapeutic advantage.