Quinizarin Gold(I) N‐Heterocyclic Carbene Complexes with Synergistic Activity Against Anthracycline‐Resistant Leukaemia Cells: Synthesis and Biological Activity Studies

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.

Institutions

Publication Details

Journal
DESY Publication Database (PUBDB) (Deutsches Elektronen-Synchrotron)
Published
2025-01-01
DOI
https://doi.org/10.3204/pubdb-2025-01683
Primary Topic
N-Heterocyclic Carbenes in Organic and Inorganic Chemistry
Type
article
Field-Weighted Citation Impact
0.00
Controls
|||
ALL TIME
JAN
FEB
MAR
APR
MAY
JUN
JUL
AUG
SEP
OCT
article

Quinizarin Gold(I) N‐Heterocyclic Carbene Complexes with Synergistic Activity Against Anthracycline‐Resistant Leukaemia Cells: Synthesis and Biological Activity Studies

DESY Publication Database (PUBDB) (Deutsches Elektronen-Synchrotron)
N-Heterocyclic Carbenes in Organic and Inorganic Chemistry
article

Quinizarin Gold(I) N‐Heterocyclic Carbene Complexes with Synergistic Activity Against Anthracycline‐Resistant Leukaemia Cells: Synthesis and Biological Activity Studies

article en

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.

DESY Publication Database (PUBDB) (Deutsches Elektronen-Synchrotron)
Deutsches Elektronen-Synchrotron DESY (DE)
Openalex Percentile: Top 68%
N-Heterocyclic Carbenes in Organic and Inorganic Chemistry
AI Navigator

Ask Laika to Summarize, Analyze, and Connect papers live on the map.

Summarize Papers & Methodologies

Extract key findings, datasets, and comparative methods across publications.

Benchmark Rankings & Visual Analytics

Rank top research institutions, authors, funders, topics, and journals by Field-Weighted Citation Impact (FWCI) and paper volume with instant charts.

Connect Distant Disciplines

Bridge topological clusters on the map to find hidden collaborative intersections.