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Effect of cyclic substituents on the anti-cancer activity and DNA interaction of ruthenium(II) bis-phenanthroline dipyridoquinoline

Lookup NU author(s): Andy Hicks, Dr Eimer TuiteORCiD

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This work is licensed under a Creative Commons Attribution 4.0 International License (CC BY 4.0).


Abstract

Copyright © 2023 Nyong-Bassey, Hicks, Bergin, Tuite, Kozhevnikov and Veuger.Introduction: Ruthenium(II) complexes have emerged recently as candidates for anti-cancer therapy, where activity is related to lipohilicity, cellular localization, and specific interactions with biomolecules. Methods: In this work, two novel complexes were synthesized and are reported based on the [Ru(phen)2(dipyrido[3,2-f:2′,3′-h]quinoxaline]2+ framework. Results: Compared to the parent complex, annealing of cyclopenteno and cyclohexeno rings to the extended ligand substantially increased cytotoxicity towards a number of cancer cell lines, and induced apoptosis. The complexes localize in the nuclei of cancer cells and co-locate with DAPI on DNA. DNA binding studies show that both complexes bind strongly to DNA and one complex intercalates DNA like the parent, whilst the other appears to have multiple modes of interaction. Discussion: It is likely that the increased lipophilicity of the novel complexes is a key factor for increasing their cytotoxicity, rather than their DNA binding mode.


Publication metadata

Author(s): Nyong-Bassey EE, Hicks AL, Bergin P, Tuite EM, Kozhevnikov V, Veuger S

Publication type: Article

Publication status: Published

Journal: Frontiers in Molecular Biosciences

Year: 2023

Volume: 10

Online publication date: 18/10/2023

Acceptance date: 27/09/2023

Date deposited: 14/11/2023

ISSN (print): 2296-889X

Publisher: Frontiers Media SA

URL: https://doi.org/10.3389/fmolb.2023.1252285

DOI: 10.3389/fmolb.2023.1252285

Data Access Statement: The original contributions presented in the study are included in the article/Supplementary Material; further inquiries can be directed to the corresponding authors.


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Funding

Funder referenceFunder name
EU H2020 MSCA RISE Grant No. 778001.

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