Novel Antitumor Cisplatin and Transplatin Derivatives Containing 1-Methyl-7-Azaindole: Synthesis, Characterization, and Cellular Responses

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F68081707%3A_____%2F15%3A00442212" target="_blank" >RIV/68081707:_____/15:00442212 - isvavai.cz</a>
Alternative codes found
RIV/61989592:15310/15:33155835
Result on the web
<a href="http://dx.doi.org/10.1021/jm501420k" target="_blank" >http://dx.doi.org/10.1021/jm501420k</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1021/jm501420k" target="_blank" >10.1021/jm501420k</a>

Result language
angličtina
Original language name
Novel Antitumor Cisplatin and Transplatin Derivatives Containing 1-Methyl-7-Azaindole: Synthesis, Characterization, and Cellular Responses
Original language description
The current work investigates the effect of new bifunctional and mononuclear Pt(II) compounds, the cis- and trans-isomers of [PtCl2(NH3)(L)] (L = 1-methyl-7-azaindole, compounds 1 and 2, respectively), on growth and viability of human carcinoma cells aswell as their putative mechanism(s) of cytotoxicity. The results show that substitution of 1-methyl-7-azaindole for ammine in cisplatin or transplatin results in an increase of the toxic efficiency, selectivity for tumor cells in cisplatin-resistant cancer cells, and activation of the trans geometry. The differences in the cytotoxic activities of 1 and 2 were suggested to be due to their different DNA binding mode, different capability to induce cell cycle perturbations, and fundamentally different roleof transcription factor p53 in their mechanism of action. Interestingly, both isomers make it possible to detect their cellular uptake and distribution in living cells by confocal microscopy without their modification with an optically a
Czech name
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Czech description
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Type
J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)
CEP classification
BO - Biophysics
OECD FORD branch
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Project
Result was created during the realization of more than one project. More information in the Projects tab.
Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Publication year
2015
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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