FOERSTROVÁ, Michaela, Zuzana JANDUROVÁ, Fernanda MARQUES, Gano LURDES, Přemysl LUBAL, Jakub VANĚK, Petr HERMANN and Isabel SANTOS. Chemical and biological evaluation of 153Sm and 166Ho complexes of 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetrakis(methylphosphonic acid monoethylester) (H4dotpOEt). Journal of Inorganic Biochemistry. Amsterdam: Elsevier Science, 2008, vol. 102, No 7, p. 1531-1540. ISSN 0162-0134.
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Basic information
Original name Chemical and biological evaluation of 153Sm and 166Ho complexes of 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetrakis(methylphosphonic acid monoethylester) (H4dotpOEt)
Name in Czech Chemické a biologické vyhodnocení 153Sm a 166Ho komplexů 1,4,7,10-tetraazacyklododekane-1,4,7,10-tetrakis(methylfosfonate monoethylester) (H4dotpOEt)
Authors FOERSTROVÁ, Michaela (203 Czech Republic), Zuzana JANDUROVÁ (203 Czech Republic), Fernanda MARQUES (620 Portugal), Gano LURDES (620 Portugal), Přemysl LUBAL (203 Czech Republic), Jakub VANĚK (203 Czech Republic), Petr HERMANN (203 Czech Republic, guarantor) and Isabel SANTOS (620 Portugal).
Edition Journal of Inorganic Biochemistry, Amsterdam, Elsevier Science, 2008, 0162-0134.
Other information
Original language English
Type of outcome Article in a journal
Field of Study 10402 Inorganic and nuclear chemistry
Country of publisher Netherlands
Confidentiality degree is not subject to a state or trade secret
Impact factor Impact factor: 3.133
RIV identification code RIV/00216224:14310/08:00026088
Organization unit Faculty of Science
UT WoS 000256924600014
Keywords in English Radiopharmaceuticals; macrocyclic and phosphonate complexes; cyclen derivative; DOTA analogue; lanthanide complexes; radiolanthanides; biodistribution; stability constants; formation and decomplexation kinetics
Tags biodistribution, Cyclen derivative, DOTA analogue, formation and decomplexation kinetics, LANTHANIDE COMPLEXES, macrocyclic and phosphonate complexes, radiolanthanides, Radiopharmaceuticals, Stability Constants
Tags International impact, Reviewed
Changed by Changed by: prof. RNDr. Přemysl Lubal, Ph.D., učo 1271. Changed: 8/4/2010 19:32.
Abstract
The novel methylphosphonic acid monoethylester (H4dotpOEt) has been synthesized and characterized and their complexes with Sm(III) and Ho(III) ions were studied. Dissociation constants of the ligand are lower than those of H4dota. The stability constants of the Ln(III)-H4dotpOEt complexes are surprisingly much lower that those of H4dota probably due to a lower coordination ability of the phosphonate monoester groups. Acid-assisted decomplexation studies have shown that both complexes are less kinetically inert than the H4dota complexes, but still much more inert than complexes of open-chain ligands. Nevertheless, the synthesis of 153Sm and 166Ho complexes with this ligand led to stable complexes both in vitro and in vivo. A very low binding of these complexes to hydroxyapatite (HA) and calcified tissues was observed confirming the assumption that a fully ionized phosphonate group(s) is necessary for a strong bone affinity. Both complexes show similar behaviour in vivo.
Abstract (in Czech)
Nový ligand "methylphosphonic acid monoethylester (H4dotpOEt)" byl syntetizován a charakterizován a jeho komplexy s Sm(III) a Ho(III) ionty byly studovány. Disociační konstanty ligandu jsou nižší než pro analogický ligand H4dota. Konstanty stability Ln(III)-H4dotpOEt komplexů jsou překvapivě nižší než ty s H4dota ligandem pravděpodobobně v důsledku menší koordinační schopnosti fosfonate- monoesterových skupin. Studie kysele-katalyzované dekomplexace ukazují, že oba komplexy jsou kineticky méně inertní než komplexy H4dota ligandu, ale stále více inertní než komplexy s ligandy mající otevřený řetězec. Syntéza 153Sm a 166Ho komplexů s tímto ligandem vedla k stabilním komplexům in vitro a in vivo. Velmi nízká schopnost vazby těchto komplexů na hydroxyapatite (HA) a zvápnětelých buněk byla pozorována a potvrdila, že plně ionizované skupiny jsou nezbytné pro silnou afinitu ke kostem. Oba komplexy ukazují podobné chování in vivo.
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