The Bulk Breast Cancer Cell and Breast Cancer Stem Cell Activity of Binuclear Copper (II)‐Phenanthroline Complexes

Abstract: Mononuclear copper (II)‐phenanthroline complexes have been widely investigated as anticancer agents whereas multinuclear copper (II)‐phenanthroline complexes are underexplored. Here the synthesis and characterisation of two new binuclear copper (II)‐phenanthroline complexes 1 and 2 is reported, comprising of 2,9‐dimethyl‐1,10‐phenanthroline or 2,9‐dimethyl‐4,7‐diphenyl‐1,10‐phenanthroline, terminal chloride ligands, and bridging chloride or hydroxide ligands. The binuclear copper (II) complex containing 2,9‐dimethyl‐1,10‐phenanthroline 1 displays nanomolar toxicity towards bulk breast cancer cells and breast cancer stem cells (CSCs) grown in monolayers, >50‐fold greater than cisplatin (an anticancer metallodrug) and salinomycin (a gold‐standard anti‐CSC agent). Spectacularly, 1 exhibits >100‐fold greater potency toward three‐dimensionally cultured mammospheres than cisplatin and salinomycin. Mechanistic studies show that 1 evokes breast CSC apoptosis by elevating intracellular reactive oxygen species levels and damaging genomic DNA (possibly by an oxidative mechanism). To the best of our knowledge, this is the first study to probe the anti‐breast CSC properties of binuclear copper (II)‐phenanthroline complexes.

Standort
Deutsche Nationalbibliothek Frankfurt am Main
Umfang
Online-Ressource
Sprache
Englisch

Erschienen in
The Bulk Breast Cancer Cell and Breast Cancer Stem Cell Activity of Binuclear Copper (II)‐Phenanthroline Complexes ; day:13 ; month:07 ; year:2023 ; extent:10
Chemistry - a European journal ; (13.07.2023) (gesamt 10)

Urheber
Osei, Priscilla B.
Northcote‐Smith, Joshua
Fang, Jiaxin
Singh, Kuldip
Ortu, Fabrizio
Suntharalingam, Kogularamanan

DOI
10.1002/chem.202301188
URN
urn:nbn:de:101:1-2023071415151586943665
Rechteinformation
Open Access; Der Zugriff auf das Objekt ist unbeschränkt möglich.
Letzte Aktualisierung
14.08.2025, 10:58 MESZ

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Beteiligte

  • Osei, Priscilla B.
  • Northcote‐Smith, Joshua
  • Fang, Jiaxin
  • Singh, Kuldip
  • Ortu, Fabrizio
  • Suntharalingam, Kogularamanan

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