Synthesis, characterization, radiolabeling and biodistribution of a novel cyclohexane dioxime derivative as a potential candidate for tumor imaging

• Published in: International journal of radiation biology 2018-06, Vol.94 (6), p.590-596
• Main Authors: Motaleb, M A, Selim, Adli A, El-Tawoosy, M, Sanad, M H, El-Hashash, M A
• Format: Article
• Language: English
• Subjects: Animals; Cell Line, Tumor; Chemistry Techniques, Synthetic; Cyclohexanes - chemical synthesis; Cyclohexanes - chemistry; Cyclohexanes - pharmacokinetics; Humans; Isotope Labeling; Mice; Molecular Imaging - methods; Oximes - chemistry; Space life sciences; Tissue Distribution
• ISSN: 0955-3002; 1362-3095
• DOI: 10.1080/09553002.2018.1466067

Dioxime derivative is reported to exhibit high affinity towards tumor cells. The objective of the present study is to synthesize a new dioxime derivative to be labeled with technetium-99m for using as a solid tumor marker. ((2E,2',3E,3')-3,3'-(cyclohexane-1,2-diylbis (azanylylidene)) bis-(butan-2-one)dioxime) was synthesized by condensation of Butan-2,3-dione monooxime and diaminocyclohexane and labeled with Tc. The in-vivo distribution of the agent was studied by carrying out biodistribution in tumor bearing Albino mice. A new cyclohexane dioxime derivative was synthesized with a good yield of 93 ± 2% and its complexation with Tc was prepared with 85 ± 4% radiochemical yield under the optimized conditions and the preparation exhibited in-vitro stability up to 6 h. Biodistribution studies showed high uptake in tumor cells with T/NT (target to non-target ratio) = 3.4 ± 0.2 after 0.5 h post injection. As a result of biodistribution studies, the newly synthesized cyclohexane dioxime derivative showed its good uptake in tumor cells, which affords a potential radiopharmaceutical that could be used as a good tumor imaging agent.