Platinum(II) carboxylato complexes containing 7-azaindoles as N-donor carrier ligands showed cytotoxicity against cancer cell lines
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61989592%3A15310%2F16%3A33161198" target="_blank" >RIV/61989592:15310/16:33161198 - isvavai.cz</a>
Result on the web
<a href="http://www.sciencedirect.com/science/article/pii/S0162013416301817" target="_blank" >http://www.sciencedirect.com/science/article/pii/S0162013416301817</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1016/j.jinorgbio.2016.06.018" target="_blank" >10.1016/j.jinorgbio.2016.06.018</a>
Alternative languages
Result language
angličtina
Original language name
Platinum(II) carboxylato complexes containing 7-azaindoles as N-donor carrier ligands showed cytotoxicity against cancer cell lines
Original language description
The platinum(II) malonato (Mal) and decanoato (Dec) complexes of the general formulas [Pt(Mal)(naza)(2)] (1-3) and cis-IPt(Dec)(2)(naza)(2)] (4-7) were prepared, characterized and tested for their in vitro cytotoxicity against cisplatin-sensitive (A2780) and cisplatin-resistant (A2780R) human ovarian carcinoma cell lines and non-cancerous human lung fibroblasts (MRC-5); naza = halogen-derivatives of 7-azaindole. Complexes 1-7 effectively overcome the acquired resistance of ovarian carcinoma cells to cisplatin. Complexes 2 (IC50 = 26.6 +/- 8.9 mu M against A2780 and 28.9 +/- 6.7 mu M against A2780R), 4 (IC50 = 14.5 +/- 0.6 mu M against A2780 and 14.5 +/- 3.8 mu M against A2780R) and 5 (IC50 = 13.0 +/- 1.1 mu M against A2780 and 13.6 +/- 4.9 mu M against A2780R) indicated decreased toxicity against healthy MRC-5 cells (IC50 > 50.0 mu M for 2 and >25.0 mu M for 4 and 5). The representative complexes 2 and 4 showed mutually different effect on the P2780 cell cycle at IC50 concentrations after 24 h exposure. Concretely, the complex 2 caused cell cycle arrest at G(0)/G(1) phase, while 4 induced cell death by apoptosis with high population of cells in sub-G(1) cell cycle phase. The hydrolysis and interactions of the selected complexes with biomolecules (glutathione (GSH) and guanosine monophosphate (GMP)) were also studied by means of H-1 NMR and ESI+ mass spectra.
Czech name
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Czech description
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Classification
Type
J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)
CEP classification
CA - Inorganic chemistry
OECD FORD branch
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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
2016
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
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Volume of the periodical
162
Issue of the periodical within the volume
SEP
Country of publishing house
US - UNITED STATES
Number of pages
18
Pages from-to
109-116
UT code for WoS article
000388059600012
EID of the result in the Scopus database
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