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Truncated fluorocyclopentenyl pyrimidines as S-adenosylhomocysteine hydrolase inhibitors
- Truncated fluorocyclopentenyl pyrimidines as S-adenosylhomocysteine hydrolase inhibitors
- Park Y.H.; Choi W.J.; Tipnis A.S.; Lee K.M.; Jeong L.S.
- Ewha Authors
- 이강만; 정낙신; 최원준
- SCOPUS Author ID
- Issue Date
- Journal Title
- Nucleosides, Nucleotides and Nucleic Acids
- vol. 28, no. 41401, pp. 601 - 613
- SCIE; SCOPUS
- On the basis of inhibitory activity of truncated cyclopentenyl cytosine against S-adenosylhomocysteine hydrolase (SAH), its fluorocyclopentenyl pyrimidine derivatives were efficiently synthesized from D-ribose via electrophilic fluorination as a key step. The final nucleosides were evaluated for SAH inhibitory activity, among which the uracil derivative 9 showed significant inhibitory activity (IC50 = 8.53 M). They were also evaluated for cytotoxic effects in several human cancer cell lines such as fibro sarcoma, stomach cancer, leukemia, and colon cancer, but they did not show any cytotoxic effects up to 100 M, indicating that 4'-hydroxymethyl groups are essential for the anticancer activity.
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