TY  - JOUR
AU  - Lakić, Mladen
AU  - Sabo, Ljubica
AU  - Ristić, Slavica
AU  - Savić, Aleksandar
AU  - Petričević, Saša
AU  - Nikolić, Nadežda
AU  - Vukadinović, Aleksandar
AU  - Janković, Drina
AU  - Sabo, Tibor
AU  - Vranješ-Đurić, Sanja
PY  - 2016
UR  - https://cherry.chem.bg.ac.rs/handle/123456789/2045
AB  - The extensive development of radiopharmaceuticals towards early tumour detection and treatment has increased the demand for new ligands with higher tumour selectivity. Research has been done on the potential of the novel O,O'-diethylethylenediamine-N,N'-di-3-propanoate (L) ligand as a radionuclide vehicle for tumour targeting. Under alkaline conditions, L hydrolyses and produces half ester ligand (L') and diacid ligand (L"), with characteristic donor atom array N, N, O. Ligand L was successfully labelled with Tc-99m at pH=9 by coordination with the octahedral fac-[Tc-99m(CO)(3)(H2O)(3)](+) intermediate, forming the main radioproduct fac-[(TcL)-Tc-99m'(CO)(3)] (Tc1). The Tc-99m complex showed a low lipophilic character (log P = 0.48) and low binding affinity to human serum albumin (2.51 +/- 0.48%). In vitro stability studies in saline and human plasma, as well as challenge studies with cysteine and histidine, revealed high stability of the complex during 24 h. Biodistribution studies of Tc1 in female C57BL/6 mice bearing B16/F1 melanoma metastases showed significant tumour uptake: 9.81 +/- 1.19% ID g(-1) in the liver, 5.87 +/- 0.54% ID g(-1) in the lungs and 3.17 +/- 0.33% ID g(-1) in the ovary at 30 min post-injection. Favourable physicochemical properties, satisfactory in vitro/in vivo stability and biodistribution profile in the experimental metastatic melanoma model indicate the possible application of the radiolabelled ligand in tumour diagnosis. Copyright (C) 2015 John Wiley & Sons, Ltd.
PB  - Wiley, Hoboken
T2  - Applied Organometallic Chemistry
T1  - Synthesis and biological evaluation of Tc-99m tricarbonyl complex of O,O '-diethylethylenediamine-N,N '-di-3-propanoate as potential tumour diagnostic agent
VL  - 30
IS  - 2
SP  - 81
EP  - 88
DO  - 10.1002/aoc.3401
ER  - 

@article{
author = "Lakić, Mladen and Sabo, Ljubica and Ristić, Slavica and Savić, Aleksandar and Petričević, Saša and Nikolić, Nadežda and Vukadinović, Aleksandar and Janković, Drina and Sabo, Tibor and Vranješ-Đurić, Sanja",
year = "2016",
abstract = "The extensive development of radiopharmaceuticals towards early tumour detection and treatment has increased the demand for new ligands with higher tumour selectivity. Research has been done on the potential of the novel O,O'-diethylethylenediamine-N,N'-di-3-propanoate (L) ligand as a radionuclide vehicle for tumour targeting. Under alkaline conditions, L hydrolyses and produces half ester ligand (L') and diacid ligand (L"), with characteristic donor atom array N, N, O. Ligand L was successfully labelled with Tc-99m at pH=9 by coordination with the octahedral fac-[Tc-99m(CO)(3)(H2O)(3)](+) intermediate, forming the main radioproduct fac-[(TcL)-Tc-99m'(CO)(3)] (Tc1). The Tc-99m complex showed a low lipophilic character (log P = 0.48) and low binding affinity to human serum albumin (2.51 +/- 0.48%). In vitro stability studies in saline and human plasma, as well as challenge studies with cysteine and histidine, revealed high stability of the complex during 24 h. Biodistribution studies of Tc1 in female C57BL/6 mice bearing B16/F1 melanoma metastases showed significant tumour uptake: 9.81 +/- 1.19% ID g(-1) in the liver, 5.87 +/- 0.54% ID g(-1) in the lungs and 3.17 +/- 0.33% ID g(-1) in the ovary at 30 min post-injection. Favourable physicochemical properties, satisfactory in vitro/in vivo stability and biodistribution profile in the experimental metastatic melanoma model indicate the possible application of the radiolabelled ligand in tumour diagnosis. Copyright (C) 2015 John Wiley & Sons, Ltd.",
publisher = "Wiley, Hoboken",
journal = "Applied Organometallic Chemistry",
title = "Synthesis and biological evaluation of Tc-99m tricarbonyl complex of O,O '-diethylethylenediamine-N,N '-di-3-propanoate as potential tumour diagnostic agent",
volume = "30",
number = "2",
pages = "81-88",
doi = "10.1002/aoc.3401"
}

Lakić, M., Sabo, L., Ristić, S., Savić, A., Petričević, S., Nikolić, N., Vukadinović, A., Janković, D., Sabo, T.,& Vranješ-Đurić, S.. (2016). Synthesis and biological evaluation of Tc-99m tricarbonyl complex of O,O '-diethylethylenediamine-N,N '-di-3-propanoate as potential tumour diagnostic agent. in Applied Organometallic Chemistry
Wiley, Hoboken., 30(2), 81-88.
https://doi.org/10.1002/aoc.3401

Lakić M, Sabo L, Ristić S, Savić A, Petričević S, Nikolić N, Vukadinović A, Janković D, Sabo T, Vranješ-Đurić S. Synthesis and biological evaluation of Tc-99m tricarbonyl complex of O,O '-diethylethylenediamine-N,N '-di-3-propanoate as potential tumour diagnostic agent. in Applied Organometallic Chemistry. 2016;30(2):81-88.
doi:10.1002/aoc.3401 .

Lakić, Mladen, Sabo, Ljubica, Ristić, Slavica, Savić, Aleksandar, Petričević, Saša, Nikolić, Nadežda, Vukadinović, Aleksandar, Janković, Drina, Sabo, Tibor, Vranješ-Đurić, Sanja, "Synthesis and biological evaluation of Tc-99m tricarbonyl complex of O,O '-diethylethylenediamine-N,N '-di-3-propanoate as potential tumour diagnostic agent" in Applied Organometallic Chemistry, 30, no. 2 (2016):81-88,
https://doi.org/10.1002/aoc.3401 . .