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Dinuclear copper(II) complexes with a bridging bis(chalcone) ligand reveal considerable in vitro cytotoxicity on human cancer cells and enhanced selectivity

The result's identifiers

  • Result code in IS VaVaI

    <a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61989592%3A15640%2F24%3A73624822" target="_blank" >RIV/61989592:15640/24:73624822 - isvavai.cz</a>

  • Alternative codes found

    RIV/61989592:15310/24:73624822

  • Result on the web

    <a href="https://www.sciencedirect.com/science/article/pii/S0162013424000047?via%3Dihub" target="_blank" >https://www.sciencedirect.com/science/article/pii/S0162013424000047?via%3Dihub</a>

  • DOI - Digital Object Identifier

    <a href="http://dx.doi.org/10.1016/j.jinorgbio.2024.112481" target="_blank" >10.1016/j.jinorgbio.2024.112481</a>

Alternative languages

  • Result language

    angličtina

  • Original language name

    Dinuclear copper(II) complexes with a bridging bis(chalcone) ligand reveal considerable in vitro cytotoxicity on human cancer cells and enhanced selectivity

  • Original language description

    A bis(chalcone) molecule (H2L) was synthesized via Aldol&apos;s condensation from terephthalaldehyde and 2 &apos; hydroxyacetophenone and it was used as bridging ligand for the preparation of five dinuclear copper(II) complexes of the composition [Cu(N-N)(mu-L)Cu(N-N)](NO3)2 &amp; sdot;nH2O (n = 0-2) (1-5), where N-N stands for a bidentate N-donor ligand such as phen (1,10-phenanthroline, 1), bpy (2,2 &apos;-bipyridine, 2), mebpy (5,5 &apos;-dimethyl2,2 &apos;-dipyridine, 3), bphen (bathophenanthroline, 4) and nphen (5-nitro-1,10-phenanthroline, 5). The compounds were characterized by different suitable techniques to confirm their purity, composition, and structure. Moreover, the products were evaluated for their in vitro cytotoxicity on a panel of human cancer cell lines: ovarian (A2780), ovarian resistant to cisplatin (A2780R), prostate (PC3), osteosarcoma (HOS), breast (MCF7) and lung (A549), and normal fibroblasts (MRC-5), showing significant cytotoxicity in most cases, with IC50 approximate to 0.35-7.8 mu M. Additionally, the time-dependent cytotoxicity and cellular uptake of copper, together with flow cytometric studies concerning cell-cycle arrest, induction of cell death and autophagy and induction of intracellular ROS/ superoxide production in A2780 cells, were also performed. The results of biological testing on A2780 cells pointed out a possible mechanism of action characterized by the G2/M cell cycle arrest and induction of apoptosis by triggering the intrinsic signalling pathway associated with the damage of mitochondrial structure and depletion of mitochondrial membrane potential.Synopsis: Dinuclear Cu(II) complexes bearing a bridging bis(chalcone) ligand revealed high in vitro cytotoxicity, initiated A2780 cell arrest at G2/M phase and efficiently triggered intrinsic pathway of apoptosis.

  • Czech name

  • Czech description

Classification

  • Type

    J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database

  • CEP classification

  • OECD FORD branch

    10402 - Inorganic and nuclear chemistry

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

    2024

  • Confidentiality

    S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Data specific for result type

  • Name of the periodical

    JOURNAL OF INORGANIC BIOCHEMISTRY

  • ISSN

    0162-0134

  • e-ISSN

    1873-3344

  • Volume of the periodical

    252

  • Issue of the periodical within the volume

    March

  • Country of publishing house

    US - UNITED STATES

  • Number of pages

    13

  • Pages from-to

  • UT code for WoS article

    001163961800001

  • EID of the result in the Scopus database

    2-s2.0-85182582405