• Journal of Life Science
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• v.9 no.1
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• pp.63-68
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• 1999

Many nucleoside compounds such as 5-halogen substituted uridine, 5'-amino-5'-deoxyuridine conjugates of amino acid, peptide, and penicillin G, 5'-monophosphate uridine derivatives and 5'-monophosphate uridine-fatty acid derivatives were chemically synthesized and their antifungal, antibacterial, and antitumor activities were tested. 5-Bromo-2',3'-O-isopropylideneuridine(6) inhibited the growth of Trichophyton rubrum at $0.2{\mu}$g/ml of MIC. 5'-Amino-5'-deoxyuridine-penicillin G(19), 5'-amino-5'-deoxyuridine-cyclo(Phe-Asp)(20), and 5-iodo-5'-amino-5'-deoxyuridine- penicillin G(22) had antibarterial activity(MIC was $6.25{\mu}$g/ml against S. aureus) and the latter two nucleoside compounds were the most antitumor derivatives(their $IC_{50}$ against L5178Y murine lymphoma cell was $6.5{\mu}$g/ml).

• The Korean Journal of Nuclear Medicine
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• v.36 no.4
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• pp.209-223
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• 2002

By considering the biological properties of a tumor, it should be possible to realize better results in cancer therapy. PET imaging offers the opportunity to measure tumor growth non-invasively and repeatedly as an early assessment of response to cancer therapy. Measuring cellular growth instead of energy metabolism showed offer significant advantages in evaluating therapy. Thymidine and its derivative nucleoside compounds can be changed to mono, di- and tri- phosphate compounds by thymidine kinase and then be incorporated into DNA. Their bindings are increased in highly proliferating cells due to the high DNA synthesis rate. To evaluate cell proliferation, many kinds of thymidine and uridine derivatives have been labeled with positron emitter and radioactive iodine. Compared to radiopharmaceuticals which have radioisotope labeled base ring such as pyirmidine, the radiopharmacuticals which have radioisotope labeled sugar ring are more stable in vivo and have metabolic resistance. The biological properties such as DNA incorporation ratios are highly dependent on their chemical structures and metabolic processes. This overview describes synthesis of radiopharmaceuticals and their biological properties for imaging of tumor cell proliferation.