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: ((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 ^99mTc. 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 ^99mTc 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.

Pyridine compounds are one of the most important heterocyclic derivatives showing wide ranges in biological and pharmacological activities. Green chemistry eliminates or reduces the generation of hazardous compounds. It prevents pollution at a molecular level. The microwave technique used in heterocyclic compound synthesis is also an important branch of green chemistry techniques. In this study, we report designing and synthesizing a new pyridine-bearing pentose moiety via a one-pot multicomponent reaction using D-glucose and also investigate its behavior and reactivity toward some simple and heterocyclic amino derivatives. The chemical structures of the synthesized compounds were characterized and tested for their cytotoxic activities. Some of the test compounds exhibited slight to high cytotoxic activities against Caco2 (colon cancer) cells, HepG2 (hepatocellular carcinoma) cells and MCF-7 (human breast cancer) cells by MTT assay. The results showed clearly that compound 4 and compound 8 displayed strongest to moderate cytotoxic activity against the HepG2, Caco2 and MCF-7 respectively and compound 1 showed good activity against MCF-7 in comparison to the standard anticancer drug doxorubicin. These data were by cytopathological examination. An in-vivo radioactive tracing study of compound 4 proved its targeting ability to sarcoma cells in a tumor-bearing mice model. Our findings suggest that the synthesized compounds may be promising candidates as novel anticancer agents.