Synthesis, characterization, radiolabeling and biodistribution of a novel cyclohexane dioxime derivative as a potential candidate for tumor imaging. (16th April 2018)

• Record Type: Journal Article
• Authors: Motaleb, M. A.; Selim, Adli A.; El-Tawoosy, M.; Sanad, M. H.; El-Hashash, M. A.
• Is Part Of: International journal of radiation biology. Volume 94:Number 6(2018)
• Page Start: 590
• Page End: 596
• Publication Date: 2018-04-16
• Subjects: Cyclohexane -- dioxime -- synthesis -- technetium-99m -- tumor imaging; Radiation -- Physiological effect -- Periodicals; Radiobiology -- Periodicals; 571.45
• DOI: 10.1080/09553002.2018.1466067
• Languages: English
• ISSNs: 0955-3002

Abstract

Abstract: Purpose: 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. Materials and methods: ((2 E, 2′, 3 E, 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 99m Tc. The in-vivo distribution of the agent was studied by carrying out biodistribution in tumor bearing Albino mice. Results: A new cyclohexane dioxime derivative was synthesized with a good yield of 93 ± 2% and its complexation with 99m 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. Conclusion: 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.