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

Kód výsledku v 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>

Výsledek na webu

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DOI - Digital Object Identifier

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Jazyk výsledku

angličtina

Název v původním jazyce

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

Popis výsledku v původním jazyce

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

Název v anglickém jazyce

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

Popis výsledku anglicky

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

Druh

J_x - Nezařazeno - Článek v odborném periodiku (Jimp, Jsc a Jost)

CEP obor

CE - Biochemie

OECD FORD obor

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Projekt

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Návaznosti

Z - Vyzkumny zamer (s odkazem do CEZ)

Rok uplatnění

2007

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

Journal of Organometallic Chemistry

ISSN

0022-328X

e-ISSN

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Svazek periodika

692

Číslo periodika v rámci svazku

6

Stát vydavatele periodika

NL - Nizozemsko

Počet stran výsledku

10

Strana od-do

1255-1264

Kód UT WoS článku

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EID výsledku v databázi Scopus

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