Reframing Triazoloacridinone C-1305 as a G-Quadruplex Pharmacophore

H NMR and UV-Vis global analysis─converge on a well-defined 2:1 Pu22:C-1305 complex with submicromolar affinity and a distinctive ligand-induced "destabilize-refold" NMR signature. Variable-temperature NMR reveals pronounced thermal stabilization of Pu22 upon binding. Intermolecular NOEs together with 3D well-tempered metadynamics map a recognition mode dominated by end-stacking on both terminal G-tetrads, with flanking segments forming secondary pockets and enabling alternative bound substates. In cell assays, C-1305 shows low-micromolar cytotoxicity across multiple cancer cell lines while being markedly less toxic to normal cells, outperforming cisplatin in potency. These results reposition C-1305 from a putative GGG intercalator to a G4-targeting pharmacophore and outline a route to side-chain engineering for improved G4 selectivity.

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Publication Details

Journal
The Journal of Physical Chemistry B
Published
2026-05-11
DOI
https://doi.org/10.1021/acs.jpcb.6c01505
Primary Topic
DNA and Nucleic Acid Chemistry
Type
article
Field-Weighted Citation Impact
0.00

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article

Reframing Triazoloacridinone C-1305 as a G-Quadruplex Pharmacophore

Monika Pawłowska, Tomasz Laskowski, Ewa Paluszkiewicz, Julia Borzyszkowska-Bukowska et al.
The Journal of Physical Chemistry B
DNA and Nucleic Acid Chemistry
article

Reframing Triazoloacridinone C-1305 as a G-Quadruplex Pharmacophore

Monika Pawłowska, Tomasz Laskowski, Ewa Paluszkiewicz, Julia Borzyszkowska-Bukowska, Karolina Zielińska, Julia Pakuła, Rafał Tomaszczyk
article en

Abstract

H NMR and UV-Vis global analysis─converge on a well-defined 2:1 Pu22:C-1305 complex with submicromolar affinity and a distinctive ligand-induced "destabilize-refold" NMR signature. Variable-temperature NMR reveals pronounced thermal stabilization of Pu22 upon binding. Intermolecular NOEs together with 3D well-tempered metadynamics map a recognition mode dominated by end-stacking on both terminal G-tetrads, with flanking segments forming secondary pockets and enabling alternative bound substates. In cell assays, C-1305 shows low-micromolar cytotoxicity across multiple cancer cell lines while being markedly less toxic to normal cells, outperforming cisplatin in potency. These results reposition C-1305 from a putative GGG intercalator to a G4-targeting pharmacophore and outline a route to side-chain engineering for improved G4 selectivity.

The Journal of Physical Chemistry B
Gdańsk University of Technology (PL), Institute of Bioorganic Chemistry, Polish Academy of Sciences (PL)
Narodowe Centrum Nauki
Openalex Percentile: Top 9%
DNA and Nucleic Acid Chemistry
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Reframing Triazoloacridinone C-1305 as a G-Quadruplex Pharmacophore — Monika Pawłowska, Tomasz Laskowski, et al. · The Journal of Physical Chemistry B (2026) | TGRS Research Map | TGRS