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- Title
Synthesis and biological evaluation of <sup>99m</sup>Tc tricarbonyl complex of O,O'-diethylethylenediamine-N,N'-di-3-propanoate as potential tumour diagnostic agent.
- Authors
Lakić, Mladen; Sabo, Ljubica; Ristić, Slavica; Savić, Aleksandar; Petričević, Saša; Nikolić, Nadežda; Vukadinović, Aleksandar; Janković, Drina; Sabo, Tibor J.; Vranješ ‐ Đurić, Sanja
- 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 atomarray N,N,O. Ligand L was successfully labelled with 99mTc at pH= 9 by coordination with the octahedral fac-[99mTc(CO)3(H2O)3]+ intermediate, forming the main radioproduct fac-[99mTcL' (CO)3] (Tc1). The 99mTc complex showed a low lipophilic character (log P = 0.48) and low binding affinity to human serumalbumin (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/6mice 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.
- Subjects
CARBONYL compounds; CHEMICAL synthesis; LIGANDS (Chemistry); METASTASIS; MELANOMA; TUMOR diagnosis
- Publication
Applied Organometallic Chemistry, 2016, Vol 30, Issue 2, p81
- ISSN
0268-2605
- Publication type
Article
- DOI
10.1002/aoc.3401