Identification of in vitro metabolites of the novel anti-tumor thiosemicarbazone, DpC, using ultra-high performance liquid chromatography-quadrupole-time-of-flight mass spectrometry

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11160%2F13%3A10146027" target="_blank" >RIV/00216208:11160/13:10146027 - isvavai.cz</a>
Result on the web
<a href="http://link.springer.com/article/10.1007/s00216-012-6562-x/fulltext.html" target="_blank" >http://link.springer.com/article/10.1007/s00216-012-6562-x/fulltext.html</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1007/s00216-012-6562-x" target="_blank" >10.1007/s00216-012-6562-x</a>

Result language
angličtina
Original language name
Identification of in vitro metabolites of the novel anti-tumor thiosemicarbazone, DpC, using ultra-high performance liquid chromatography-quadrupole-time-of-flight mass spectrometry
Original language description
Di-2-pyridylketone-4-cyclohexyl-4-methyl-3-thiosemicarbazone (DpC) is a promising analogue of the dipyridyl thiosemicarbazone class currently under development as a potential anti-cancer drug. In fact, this class of agents shows markedly greater anti-tumor activity and selectivity than the clinically investigated thiosemicarbazone, Triapine(R). However, further development of DpC requires detailed data concerning its metabolism. Therefore, we focused on the identification of principal phase I and II metabolites of DpC in vitro. DpC was incubated with human liver microsomes/S9 fractions and the samples were analyzed using ultra-performance liquid chromatography (UPLC(TM)) with electrospray ionization quadrupole-time-of-flight (Q-TOF) mass spectrometry.An Acquity UPLC BEH C-18 column was implemented with 2 mM ammonium acetate and acetonitrile in gradient mode as the mobile phase. The chemical structures of metabolites were proposed based on the accurate mass measurement of the protonate
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
CB - Analytical chemistry, separation
OECD FORD branch
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Project
<a href="/en/project/NT12403" target="_blank" >NT12403: Pharmaceutical analysis, pharmacokinetic and biotransformation study of novel thiosemicarbazone anticancer drugs</a><br>
Continuities
S - Specificky vyzkum na vysokych skolach<br>I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Publication year
2013
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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