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Is antitumor Pt(IV) complex containing two axial lonidamine ligands a true dual- or multi-action prodrug?

The result's identifiers

  • Result code in IS VaVaI

    <a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F68081707%3A_____%2F22%3A00559611" target="_blank" >RIV/68081707:_____/22:00559611 - isvavai.cz</a>

  • Result on the web

    <a href="https://academic.oup.com/metallomics/article/14/7/mfac048/6618656?login=true" target="_blank" >https://academic.oup.com/metallomics/article/14/7/mfac048/6618656?login=true</a>

  • DOI - Digital Object Identifier

    <a href="http://dx.doi.org/10.1093/mtomcs/mfac048" target="_blank" >10.1093/mtomcs/mfac048</a>

Alternative languages

  • Result language

    angličtina

  • Original language name

    Is antitumor Pt(IV) complex containing two axial lonidamine ligands a true dual- or multi-action prodrug?

  • Original language description

    This work studied the mechanism of action of a Pt(IV) complex 2 bearing two axial lonidamine ligands, which are selective inhibitors of aerobic glycolysis. The presence of two lonidamine ligands in 2 compared to the parent Pt(II) complex increased its antiproliferative activity, cellular accumulation, and changed its cell cycle profile and mechanism of cell death. In 3D cell culture, 2 showed exceptional antiproliferative activity with IC50 values as low as 1.6 mu M in MCF7 cells. The study on the influence of the lonidamine ligands in the Pt complex on glycolysis showed only low potency of ligands to affect metabolic processes in cancer cells, making the investigated complex, not a dual- or multi-action prodrug. However, the Pt(IV) prodrug effectively delivers the cytotoxic Pt(II) complex into cancer cells.

  • 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

    10608 - Biochemistry and molecular biology

Result continuities

  • Project

    <a href="/en/project/GC20-14082J" target="_blank" >GC20-14082J: Development of new, targeting polynuclear platinum and ruthenium complexes for anticancer chemotherapy. Mechanism of action</a><br>

  • Continuities

    I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Others

  • Publication year

    2022

  • Confidentiality

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

Data specific for result type

  • Name of the periodical

    Metallomics

  • ISSN

    1756-5901

  • e-ISSN

    1756-591X

  • Volume of the periodical

    14

  • Issue of the periodical within the volume

    7

  • Country of publishing house

    GB - UNITED KINGDOM

  • Number of pages

    12

  • Pages from-to

    mfac048

  • UT code for WoS article

    000827780700001

  • EID of the result in the Scopus database

    2-s2.0-85134721431