Gold(I) N-Heterocyclic Carbene Complexes with 7-Azaindoles Demonstrates In Vitro Antiproliferative Effects on Ovarian Cancer Cells and Anti-inflammatory Activity
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61989592%3A15640%2F24%3A73625468" target="_blank" >RIV/61989592:15640/24:73625468 - isvavai.cz</a>
Alternative codes found
RIV/61989592:15310/24:73625468
Result on the web
<a href="https://pubs.acs.org/doi/10.1021/acs.organomet.4c00093?ref=PDF" target="_blank" >https://pubs.acs.org/doi/10.1021/acs.organomet.4c00093?ref=PDF</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1021/acs.organomet.4c00093" target="_blank" >10.1021/acs.organomet.4c00093</a>
Alternative languages
Result language
angličtina
Original language name
Gold(I) N-Heterocyclic Carbene Complexes with 7-Azaindoles Demonstrates In Vitro Antiproliferative Effects on Ovarian Cancer Cells and Anti-inflammatory Activity
Original language description
The gold(I) N-heterocyclic carbene (NHC) complexes, containing a combination of 1,3-bis(2,6-diisopropylphenyl)imidazole-2-ylidene (iPr) and the corresponding 7-azaindole derivative (HL1-4), were prepared and characterized. The complexes of the composition of [Au(iPr)(Ln)], where n = 1-4 for 5-fluoro-7-azaindole (1), 5-bromo-7-azaindole (2), 3-chloro-7-azaindole (3), and 3-iodo-7-azaindole (4), were further evaluated for their in vitro anticancer and anti-inflammatory activities. The results showed that complexes (1-4) behave as considerably cytotoxic against human ovarian cancer cell line A2780 (with IC50 approximate to 4-9 mu M) and cisplatin-resistant cell line A2780R (with IC50 approximate to 7-12 mu M, except for 2 with IC50 > 25 mu M), providing significantly higher cytotoxicity than the anticancer drug cisplatin. Moreover, they also revealed a relatively good selectivity over normal cells (MRC-5), with selectivity index values of SI > 2.5. Complex 4 showed the ability to interact with l-cysteine and reduced glutathione at normal extracellular and intracellular levels, respectively. Complex 4 was further studied for its cellular effects in A2780 cells using flow cytometry. The ability of complexes (1-4) to influence the activity of pro-inflammatory transcription factor NF-kappa B and secretion of TNF-alpha were evaluated, showing that complex 4 reveals comparable effects as the inflammatory drug auranofin.
Czech name
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Czech description
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Classification
Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
10402 - Inorganic and nuclear chemistry
Result continuities
Project
<a href="/en/project/GF21-38204L" target="_blank" >GF21-38204L: Complexes of selected transition metals with plant-derived compounds with anti-NF-kappa B and pro-PPAR dual activities</a><br>
Continuities
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)
Others
Publication year
2024
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
ORGANOMETALLICS
ISSN
0276-7333
e-ISSN
1520-6041
Volume of the periodical
43
Issue of the periodical within the volume
10
Country of publishing house
US - UNITED STATES
Number of pages
10
Pages from-to
"1155 "- 1164
UT code for WoS article
001225215800001
EID of the result in the Scopus database
2-s2.0-85193279008