Synthesis, in vitro and in silico assessment of organometallic Rhenium(I) and Technetium(I) thymidine complexes

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60461373%3A22330%2F07%3A00019132" target="_blank" >RIV/60461373:22330/07:00019132 - isvavai.cz</a>
Result on the web
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DOI - Digital Object Identifier
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Result language
angličtina
Original language name
Synthesis, in vitro and in silico assessment of organometallic Rhenium(I) and Technetium(I) thymidine complexes
Original language description
Thymidine kinases have been identified as suitable targets for noninvasive imaging of gene therapy and cancer. Thus, there is a high interest in new, reliable and inexpensive radiolabeled thymidine analogues for these applications. In this study we present the synthesis and in vitro evaluation of M(CO)(3)complexes of thymidine (M = Tc99m, Re) for potential use in SPECT tumor imaging. 5'amino5' deoxythymidine was derivatized at position C5' with spacers of various lengths (similar to 030 angstrom) carrying tridentate metal chelating entities such as iminodiacetic acid and picolylamineNmonoacetic acid. The nucleoside derivatives were reacted with the precursors [ReBr3(CO)(3)](2) and [Tc99m(OH2)(3)(CO)(3)](+), respectively. The organometallic thymidine complexes have been fully characterized by means of IR, NMR and mass spectrometry. Enzyme kinetic studies revealed mixed inhibition of the human cytosolic thymidine kinase with Ki values ranging from 4.4 to 334 mu M for all thymidine c
Czech name
Synthesis, in vitro and in silico assessment of organometallic Rhenium(I) and Technetium(I) thymidine complexes
Czech description
Byly připraveny značené (Tc, Re) ligandy thymidin kinasy

Type
J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)
CEP classification
CE - Biochemistry
OECD FORD branch
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Publication year
2007
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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