TRUNCATED FLUOROCYCLOPENTENYL PYRIMIDINES AS S-ADENOSYLHOMOCYSTEINE HYDROLASE INHIBITORS

被引：5
作者：
Park, Yeon Hee
Choi, Won Jun
Tipnis, Arnol S.
Lee, Kang Man
Jeong, Lak Shin
机构：
[1] Ewha Womans Univ, Dept Bioinspired Sci, Seoul 120750, South Korea
[2] Ewha Womans Univ, Div Life & Pharmaceut Sci, Coll Pharm, Seoul 120750, South Korea
来源：
NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS | 2009年 / 28卷 / 5-7期
关键词：
Truncated nucleosides; S-adenosylhomocysteine hydrolase; electrophilic fluorination; L-HOMOCYSTEINE HYDROLASE; CARBOCYCLIC NUCLEOSIDES; NEPLANOCIN-A; DERIVATIVES; ANTITUMOR; DESIGN;
D O I：
10.1080/15257770903054316
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
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 mu 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 mu M, indicating that 4'-hydroxymethyl groups are essential for the anticancer activity.
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收藏
页码：601 / 613
页数：13
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