Contribution to a conference proceedings/Journal Article

PUBDB-2025-01683

http://join2-wiki.gsi.de/foswiki/pub/Main/Artwork/join2_logo100x88.png Quinizarin Gold(I) N‐Heterocyclic Carbene Complexes with Synergistic Activity Against Anthracycline‐Resistant Leukaemia Cells: Synthesis and Biological Activity Studies

Steinbrueck, A. ; Reback, M. L. ; Rumancev, C. ; Siegmund, D. ; Garrevoet, J.DESY* ; Falkenberg, G.DESY* ; Rosenhahn, A.Extern* ; Prokop, A. ; Metzler-Nolte, N. (Corresponding author)

2025
Wiley-VCH Weinheim

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Please use a persistent id in citations: doi:10.1002/chem.202404147  doi:10.3204/PUBDB-2025-01683

Abstract: New, asymmetric quinizarin-Au(I)-NHC complexes were designed, isolated, and fully characterised including by single crystal X-ray crystallography. Cytotoxicity studies showed effective growth inhibition in HeLa cervical cancer cells with IC$_{50}$ values ranging from 2.4 μM to 5.3 μM. The successful cellular uptake was evidenced by X-ray fluorescence imaging on cryo-preserved whole HeLa cells and the sub-cellular localisation was monitored by live-cell fluorescence microscopy. Notably, complex 2 b showed circumvention of acquired anthracycline resistance in K562 leukaemia cells as well as synergistic activity with doxorubicin against both wild-type and anthracycline-resistant Nalm-6 leukaemia cells. Interestingly, sub-cellular localisation towards mitochondria proved to be more important than the compounds’ overall cytotoxicity for potent antiproliferative activity and to achieve effective resistance circumvention.

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Contributing Institute(s):

1. FS DOOR-User (FS DOOR-User)
2. Experimentebetreuung PETRA III (FS-PET-S)

Research Program(s):

1. 633 - Life Sciences – Building Blocks of Life: Structure and Function (POF4-633) (POF4-633)
2. 6G3 - PETRA III (DESY) (POF4-6G3) (POF4-6G3)
3. DFG project G:(GEPRIS)518777768 - Entwicklung von Sonden für das selektive Anfärben intrazellulärer Organelle in der Röntgenfluoreszenzspektroskopie von menschlichen Zell- und Gewebeproben (518777768) (518777768)

Experiment(s):

1. PETRA Beamline P06 (PETRA III)

Appears in the scientific report 2025

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Database coverage:
; ; ; Chemical Reactions ; Clarivate Analytics Master Journal List ; Current Contents - Physical, Chemical and Earth Sciences ; DEAL Wiley ; Ebsco Academic Search ; Essential Science Indicators ; IF < 5 ; Index Chemicus ; JCR ; Nationallizenz ; SCOPUS ; Science Citation Index Expanded ; Web of Science Core Collection

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