Heteroleptic Copper(II) Complexes Containing 2′-Hydroxy-4-(Dimethylamino)Chalcone Show Strong Antiproliferative Activity
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61989592%3A15640%2F23%3A73620094" target="_blank" >RIV/61989592:15640/23:73620094 - isvavai.cz</a>
Alternative codes found
RIV/61989592:15310/23:73620094
Result on the web
<a href="https://www.mdpi.com/1999-4923/15/2/307" target="_blank" >https://www.mdpi.com/1999-4923/15/2/307</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.3390/pharmaceutics15020307" target="_blank" >10.3390/pharmaceutics15020307</a>
Alternative languages
Result language
angličtina
Original language name
Heteroleptic Copper(II) Complexes Containing 2′-Hydroxy-4-(Dimethylamino)Chalcone Show Strong Antiproliferative Activity
Original language description
A series of six heteroleptic copper(II) complexes with 2 '-hydroxy-4-(dimethylamino)chalcone (HL) with the composition [Cu(N-N)(L)]NO3 (1-6), where N-N stands for dmbpy = 5,5 '-dimethyl-2,2 '-bipyridine (1), bphen = 4,7-diphenyl-1,10-phenanthroline (2), dbbpy = 4,4 '-di-tert-butyl-2,2 '-bipyridine (3), nphen = 5-nitro-1,10-phenanthroline (4), bpy = 2,2 '-bipyridine, (5), and dpa = 2,2 '-dipyridylamine (6), was prepared and thoroughly characterized. The in vitro cytotoxicity screening on eight human cancer cell lines identified complex 2, containing the bulkiest N-donor ligands (bphen) as highly cytotoxic against cancer cells, with IC50 values ranking from 1.0 to 2.3 mu M, with good selectivity and low toxicity against healthy human fetal lung fibroblasts MRC-5. The cell-based assays, involving the most effective complex 2 in A2780 cancer cells, revealed its strong pro-apoptotic effects based on the effective activation of caspases 3/7, ROS overproduction, and autophagy in the A2780 cells while not impeding the cell cycle and mitochondrial membrane functions. The cellular uptake studies in A2780 and 22Rv1 cells uncovered no intracellular transport of the cationic complex 2, supporting the hypothesis that the in vitro anticancer effects of complex 2 are based on the combined extrinsic activation of apoptosis and autophagy induction.
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
21002 - Nano-processes (applications on nano-scale); (biomaterials to be 2.9)
Result continuities
Project
Result was created during the realization of more than one project. More information in the Projects tab.
Continuities
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)
Others
Publication year
2023
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
Pharmaceutics
ISSN
1999-4923
e-ISSN
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Volume of the periodical
15
Issue of the periodical within the volume
2
Country of publishing house
CH - SWITZERLAND
Number of pages
21
Pages from-to
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UT code for WoS article
000940911000001
EID of the result in the Scopus database
2-s2.0-85149115450