Uridine Nucleoside 유도체의 합성과 생물 활성

Syntheses and Biological Activities of Uridine Nucleoside Derivatives

5-halogen substituted uridine, amino acid, peptide 및 penicillin G의 5'-amino -5' -deoxyuridine con-jugates, 5'-monophosphate uridine 유도체, 5'-monophosphate uridine -fat쇼 acid 유도체와 같은 nu-cleoside 화합물들을 화학적으로 합성한 후 이들의 항진균, 항균 및 항암 활성을 측정하였다. 5-Bromo-2',3'-O-isopropylideneuridine(6)은 Trichophyton rubrum의 성장을 억제하였다(MIC: $0.2{\mu}$g/ml). 5'-Amino-5' -deoxyuridine -penicillin G(19), 5'-amino-5'-deoxyuridine-cyclo(Phe -Asp)(20), 5-iodo-5'-amino -5' -deoxyuridine-penicillin G(22)는 항균적이었고(S. aureus에 대해 MIC가 $6.25{\mu}$g/ml) 뒤의 두 nucleoside 화합물은 항암 작용이 가장 강한 유도체이었다(L5178Y murine lymphoma cell에 대한 $IC_{50}$이 $6.5{\mu}$g/ml).

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).