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A. R. Jalilian, Mahdi Sadeghi, Yari Y. Kamrani

Development of [¹⁰³Pd]-labeled-bis(N⁴-methylthiosemicarbazone) complexes as possible therapeutic agents

Keywords: Palladium-103, Palladium(II) complexes, Radiolabeling, bis-thiosemicarbazono complexes, PTSM

Due to interesting tumor seeking properties of bis
-thiosemicarbazones, two radio palladium- bis -thiosemicarbazone complexes, i.e. , [ ¹⁰³Pd]-pyruvaldehyde- bis(N⁴-methylthiosemicarbazone) ([ ¹⁰³Pd] PTSM) and [ ¹⁰³Pd]- di-acetyl-bis (N⁴-methylthiosemicarbazone) ([ ¹⁰³Pd]ATSM) were prepared according to the analogy of radio copper homologs. Palladium-103 (t_1/2=16.96 d) was produced via the ¹⁰³Rh(p,n) ¹⁰³Pd nuclear reaction with proton energy 18 MeV. The final activity was eluted in form of Pd(NH₃)₂Cl₂ in order to react with bis -thiosemicarbazones to yield [ ¹⁰³Pd]-labeled compounds. Chemical purity of the product was confirmed to be below the accepted limits by polarography. [ ¹⁰³Pd]-labeled bis -thiosemicarbazones were prepared with a radiochemical yield of more than 80% at room temperature after 60–90 min by vortexing a mixture of thiosemicarbazones and Pd activity in ethanol. The purification of the labeled compounds performed by reverse phase column chromatography using C₁₈ plus Sep-Pak. Radiochemical purity of more than 99% specific activity of about 12500–13000 Ci/mol was obtained. The stability of the complexes was checked in final product and presence of human serum at 37 °C up to 48 h. The partition co-efficients of the final complexes were determined. The initial physico-chemical properties of the labeled compounds were compared to those of their copper homologues.

Radiochimica Acta, Oldenbourg Wissenschaftsverlag

Print ISSN: 0033-8230
Volume: 94, 12/2006
Pages: 865 - 869

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