In vitro anticancer active cis-Pt(II)-diiodido complexes containing 4-azaindoles
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61989592%3A15310%2F19%3A73596661" target="_blank" >RIV/61989592:15310/19:73596661 - isvavai.cz</a>
Result on the web
<a href="https://link.springer.com/article/10.1007%2Fs00775-019-01643-8" target="_blank" >https://link.springer.com/article/10.1007%2Fs00775-019-01643-8</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1007/s00775-019-01643-8" target="_blank" >10.1007/s00775-019-01643-8</a>
Alternative languages
Result language
angličtina
Original language name
In vitro anticancer active cis-Pt(II)-diiodido complexes containing 4-azaindoles
Original language description
4-Azaindole (1H-pyrrolo[3,2-b]pyridine; 4aza) and its N1-alkylated derivative N1-isopropyl-4-azaindole (1-(propan-2-yl)-1H-pyrrolo[3,2-b]pyridine; ip4aza) have been used for the preparation of the cis-diiodido-platinum(II) complexes cis-[Pt(4aza)(2)I-2] (1), cis-[PtI2(ip4aza)(2)] (2), cis-[Pt(4aza)I-2(NH3)] (3) and cis-[PtI2(ip4aza)(NH3)] (4). The prepared complexes were thoroughly characterized (e.g., multinuclear NMR spectroscopy and ESI mass spectrometry) and their in vitro cytotoxicity was assessed at human ovarian carcinoma (A2780), cisplatin-resistant ovarian carcinoma (A2780R) and colon carcinoma (HT-29) cell lines, where they showed, in some cases, significantly higher activity than the used reference-drug cisplatin. The results of in vitro cytotoxicity testing at the A2780 and A2780R cells indicated that alkylation of the 4-azaindole moiety at the position of the N1 atom had a positive biological effect, because the ip4aza-containing complexes 2 and 4 showed significantly (p<0.005) higher cytotoxicity than 4aza-containing analogues 1 and 3. The resistance factors (A2780R/A2780 model) equalled 0.8-1.4, indicating the ability of complexes 1-4 to overcome the acquired resistance of the A2780 cells against cisplatin. Complexes 1 and 2 revealed low toxicity against primary culture of human hepatocytes. The flow cytometry studies of the A2780 cell cycle modification showed that complexes 1-4 induce different cell cycle perturbations as compared with cisplatin, thus suggesting a different mechanism of their antitumor action.
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
10402 - Inorganic and nuclear chemistry
Result continuities
Project
<a href="/en/project/LO1305" target="_blank" >LO1305: Development of the center of advanced technologies and materials</a><br>
Continuities
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)<br>S - Specificky vyzkum na vysokych skolach
Others
Publication year
2019
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 BIOLOGICAL INORGANIC CHEMISTRY
ISSN
0949-8257
e-ISSN
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Volume of the periodical
24
Issue of the periodical within the volume
2
Country of publishing house
DE - GERMANY
Number of pages
13
Pages from-to
257-269
UT code for WoS article
000460591600010
EID of the result in the Scopus database
2-s2.0-85061569661