All

What are you looking for?

All
Projects
Results
Organizations

Quick search

  • Projects supported by TA ČR
  • Excellent projects
  • Projects with the highest public support
  • Current projects

Smart search

  • That is how I find a specific +word
  • That is how I leave the -word out of the results
  • “That is how I can find the whole phrase”

Half-Sandwich Ir(III) Complex of N1-Pyridyl-7-azaindole Exceeds Cytotoxicity of Cisplatin at Various Human Cancer Cells and 3D Multicellular Tumor Spheroids

The result's identifiers

  • Result code in IS VaVaI

    <a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61989592%3A15310%2F18%3A73591068" target="_blank" >RIV/61989592:15310/18:73591068 - isvavai.cz</a>

  • Result on the web

    <a href="https://pubs.acs.org/doi/pdf/10.1021/acs.organomet.8b00415" target="_blank" >https://pubs.acs.org/doi/pdf/10.1021/acs.organomet.8b00415</a>

  • DOI - Digital Object Identifier

    <a href="http://dx.doi.org/10.1021/acs.organomet.8b00415" target="_blank" >10.1021/acs.organomet.8b00415</a>

Alternative languages

  • Result language

    angličtina

  • Original language name

    Half-Sandwich Ir(III) Complex of N1-Pyridyl-7-azaindole Exceeds Cytotoxicity of Cisplatin at Various Human Cancer Cells and 3D Multicellular Tumor Spheroids

  • Original language description

    The half-sandwich iridium(III) complexes [Ir-(eta(5)-Cp-x)(phaza(-))Cl] (1, 2), [Ir(eta(5)-Cp-x)(thaza(-))Cl] (3, 4), and [Ir(eta(5)-Cp-x)(pyaza)Cl]PF6 (5, 6) containing deprotonated 1-phenyl-7-azaindole (phaza(-)) and 1-(thiophen-2-yl)-7-azaindole (thaza(-)) and electroneutral 1-(pyridin-2-yl)-7-azaindole (pyaza), were prepared; Cp-x = pentamethylcyclopentadienyl (Cp*; for 1, 3, and 5) or 1,2,3,4-tetramethyl-5-phenyl-cyclopentadienyl (Cp-Ph; for 2, 4, and 6). The complexes were thoroughly characterized, including a single-crystal X-ray analysis of complexes 1, 5, and 6. All of the complexes were screened for their in vitro cytotoxicity at the A2780 human ovarian carcinoma cell line and its A2780R cisplatin-resistant variant (2D culture cells). The best-performing complex 6 was further studied against the human DU-145 prostatic carcinoma, A549 lung carcinoma, HCT116 colon carcinoma, HeLa cervix adenocarcinoma, and MCF7 breast adenocarcinoma cell lines (2D culture cells). Complex 6 showed a cytotoxic profile different from that of cisplatin at the used cells, with the highest activity detected at the A2780, MCF7, and HCT116 cells (IC50 = 3.1, 6.9, and 10.4 mu M, respectively). Complex 6 exhibited relevant selectivity toward cancer cells (IC50 = 3.1-13.0 mu M) over the MRC-5 human noncancerous lung fibroblast cells (IC50 &gt; 50.0 mu M). Complex 6 was markedly more accumulated by the A2780 cells in comparison to cisplatin after 24 h exposure. Flow cytometry studies showed that the cell cycle of the A2780 cells treated by complex 6 is modified differently (G(0)/G(1), arrest) in comparison to cisplatin (G(2)/M arrest). Additionally to the monolayer (2D) cancer cell cultures, the cytotoxicity of complex 6 was for the first time among half-sandwich iridium(III) complexes also assessed at spheroid (3D) MCF7 cells, where its potency (IC50 = 22.9 mu M for complex 6) remained significantly better than that for the reference drug cisplatin (IC50 = 35.4 mu M).

  • 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

    2018

  • Confidentiality

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

Data specific for result type

  • Name of the periodical

    ORGANOMETALLICS

  • ISSN

    0276-7333

  • e-ISSN

  • Volume of the periodical

    37

  • Issue of the periodical within the volume

    16

  • Country of publishing house

    US - UNITED STATES

  • Number of pages

    11

  • Pages from-to

    2749-2759

  • UT code for WoS article

    000443526200013

  • EID of the result in the Scopus database

    2-s2.0-85052704111