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Truncated fluorocyclopentenyl pyrimidines as S-adenosylhomocysteine hydrolase inhibitors

Title
Truncated fluorocyclopentenyl pyrimidines as S-adenosylhomocysteine hydrolase inhibitors
Authors
Park Y.H.Choi W.J.Tipnis A.S.Lee K.M.Jeong L.S.
Ewha Authors
이강만정낙신최원준
SCOPUS Author ID
이강만scopus
Issue Date
2009
Journal Title
Nucleosides, Nucleotides and Nucleic Acids
ISSN
1525-7770JCR Link
Citation
vol. 28, no. 41401, pp. 601 - 613
Indexed
SCIE; SCOPUS WOS scopus
Abstract
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.
DOI
10.1080/15257770903054316
Appears in Collections:
약학대학 > 약학과 > Journal papers
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