Structurally diverse zinc(II) complexes containing tripodal tetradentate phenoxido-amines with promising antiproliferative effects
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61989592%3A15310%2F24%3A73625469" target="_blank" >RIV/61989592:15310/24:73625469 - isvavai.cz</a>
Alternative codes found
RIV/61989592:15640/24:73625469
Result on the web
<a href="https://pubs.rsc.org/en/content/articlelanding/2024/dt/d4dt00942h" target="_blank" >https://pubs.rsc.org/en/content/articlelanding/2024/dt/d4dt00942h</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1039/d4dt00942h" target="_blank" >10.1039/d4dt00942h</a>
Alternative languages
Result language
angličtina
Original language name
Structurally diverse zinc(II) complexes containing tripodal tetradentate phenoxido-amines with promising antiproliferative effects
Original language description
Structurally diverse zinc(II) complexes with tripodal tetradentate phenolic-amines of variable substituents in the phenol and amine moieties were synthesized and thoroughly characterized. The two dinuclear [Zn-2(L-1)(2)](ClO4)(2)MeOH (1), [Zn-2(L-2)(2)](ClO4)(2) (2), and four mononuclear [Zn(L-3)(H2O)]MeOH (3), [Zn(L-4)] (4), [Zn(L-5)] (5) and [Zn(L-6)] (6) complexes revealed distorted octahedral, trigonal-bipyramidal or tetrahedral geometries. The free HL1 and H2L3-6 ligands, and complexes 1-6 were evaluated for in vitro cytotoxicity against human cancer cell lines (A2780, A2780R, PC-3 and 22Rv1) and normal healthy MRC-5 cells. Overall results revealed high-to-moderate cytotoxicity (with the best IC50 values for complex 6 ranging from 2.4 to 4.5 mu M), which is however, significantly higher than that of the reference drug cisplatin. The moderately active complexes 1-4 showed considerable selectivity on A2780 cells (IC50 approximate to 16.3-19.5 mu M) over MRC-5 ones (with IC50 >50 mu M for 1, 2 and 4, and with IC50 >25 mu M for 3). The complexes 1, 2, and 6 and the ligand H2L6 were chosen for subsequent deeper biological evaluations. Their time-resolved cellular uptake and other cellular effects in A2780 cells were studied, such as cell cycle profile, intracellular ROS production, induction of apoptosis and activation of caspases 3/7. Complexes 1 and 2 caused significant G0/G1 cell cycle arrest in A2780 cells and antioxidant effects at normal conditions. They showed only limited effects on cellular processes connected with cytotoxicity, i.e. induction of apoptosis, depletion of mitochondrial membrane potential, and autophagy. These findings can be at least partly attributed to the low ability of the complexes to enter the A2780 cells and the depression of metabolic activity of the target cancer cells.
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
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Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace
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
Dalton Transactions
ISSN
1477-9226
e-ISSN
1477-9234
Volume of the periodical
53
Issue of the periodical within the volume
29
Country of publishing house
GB - UNITED KINGDOM
Number of pages
20
Pages from-to
"12261 "- 12280
UT code for WoS article
001268308800001
EID of the result in the Scopus database
2-s2.0-85198054281