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Updated: May 21, 2026

In Vitro Chemical Mapping of G-Quadruplex DNA Structures by Bis-3-Chloropiperidines
Published on: May 12, 2023
Synthesis, DNA-binding and antiproliferative properties of acridine and 5-methylacridine derivatives
Rubén Ferreira1, Anna Aviñó, Stefania Mazzini
1Institute for Research in Biomedicine, Baldiri Reixac 10, E-08028 Barcelona, Spain. ruben.ferreira@irbbarcelona.org
Abstract:
Several acridine derivatives were synthesized and their anti-proliferative activity was determined. The most active molecules were derivatives of 5-methylacridine-4-carboxylic acid. The DNA binding properties of the synthesized acridines were analyzed by competitive dialysis and compared with the anti-proliferative activities. While inactive acridine derivatives showed high selectivity for G-quadruplex structures, the most active 5-methylacridine-4-carboxamide derivatives had high affinity for DNA but showed poor specificity. An NMR titration study was performed with the most active 5-methylacridine-4-carboxamide, confirming the high affinity of this compound for both duplex and quadruplex DNAs.
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