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Platinum(IV) Derivatives of [Pt(1<i>S</i>,2<i>S</i>-diaminocyclohexane)(5,6-dimethyl-1,10-phenanthroline)] with Diclofenac Ligands in the Axial Positions: A New Class of Potent Multi-action Agents Exhibiting Selectivity to Cancer Cells

The result's identifiers

  • Result code in IS VaVaI

    <a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F68081707%3A_____%2F23%3A00583634" target="_blank" >RIV/68081707:_____/23:00583634 - isvavai.cz</a>

  • Result on the web

    <a href="https://pubs.acs.org/doi/10.1021/acs.jmedchem.3c00269" target="_blank" >https://pubs.acs.org/doi/10.1021/acs.jmedchem.3c00269</a>

  • DOI - Digital Object Identifier

    <a href="http://dx.doi.org/10.1021/acs.jmedchem.3c00269" target="_blank" >10.1021/acs.jmedchem.3c00269</a>

Alternative languages

  • Result language

    angličtina

  • Original language name

    Platinum(IV) Derivatives of [Pt(1<i>S</i>,2<i>S</i>-diaminocyclohexane)(5,6-dimethyl-1,10-phenanthroline)] with Diclofenac Ligands in the Axial Positions: A New Class of Potent Multi-action Agents Exhibiting Selectivity to Cancer Cells

  • Original language description

    The platinum(II) complex [Pt(1S,2S-diaminocyclohexane)(5,6-dimethyl-1,10-phenanthroline)](2+) (Pt(II)56MeSS, 1) exhibits high potencyacross numerous cancer cell lines acting by a multimodal mechanism.However, 1 also displays side toxicity and in vivo activity,all details of its mechanism of action are not entirely clear. Here,we describe the synthesis and biological properties of new platinum(IV)prodrugs that combine 1 with one or two axially coordinatedmolecules of diclofenac (DCF), a non-steroidal anti-inflammatory cancer-selectivedrug. The results suggest that these Pt(IV) complexes exhibit mechanismsof action typical for Pt(II) complex 1 and DCF, simultaneously.The presence of DCF ligand(s) in the Pt(IV) complexes promotes theantiproliferative activity and selectivity of 1 by inhibitinglactate transporters, resulting in blockage of the glycolytic processand impairment of mitochondrial potential. Additionally, the investigatedPt(IV) complexes selectively induce cell death in cancer cells, andthe Pt(IV) complexes containing DCF ligands induce hallmarks of immunogeniccell death in 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

    10402 - Inorganic and nuclear chemistry

Result continuities

  • Project

    <a href="/en/project/GA21-27514S" target="_blank" >GA21-27514S: Metal-based compounds for enhanced cancer immunotherapy</a><br>

  • Continuities

    I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

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

    Journal of Medicinal Chemistry

  • ISSN

    0022-2623

  • e-ISSN

    1520-4804

  • Volume of the periodical

    66

  • Issue of the periodical within the volume

    12

  • Country of publishing house

    US - UNITED STATES

  • Number of pages

    15

  • Pages from-to

    7894-7908

  • UT code for WoS article

    001006562300001

  • EID of the result in the Scopus database

    2-s2.0-85163517797