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Design, synthesis, and anti-tumor activity of 4′-thionucleosides as potent and selective agonists at the human A3 adenosine receptor

Title
Design, synthesis, and anti-tumor activity of 4′-thionucleosides as potent and selective agonists at the human A3 adenosine receptor
Authors
Jeong L.S.Lee H.W.Kim H.O.Jung J.Y.Gunaga P.Lee S.K.Lee E.-J.Chun M.W.Gao Z.-G.Jacobson K.A.Moon H.R.
Ewha Authors
정낙신이상국
Issue Date
2007
Journal Title
Nucleosides, Nucleotides and Nucleic Acids
ISSN
1525-7770JCR Link
Citation
vol. 26, no. 41559, pp. 1565 - 1568
Indexed
SCIE; SCOPUS WOS scopus
Abstract
On the basis of potent and selective binding affinity of Cl-IB-MECA to the human A3 adenosine receptor, its 4′-thioadenosine derivatives were efficiently synthesized starting from D-gulonic γ -lactone. Among compounds tested, 2-chloro-N6-(3-iodobenzyl)- and 2-chloro-N 6-methyl-4′ -thioadenosine-5′ -methyluronamides (7a and 7b) exhibited nanomolar range of binding affinity (Ki = 0.38 nM and 0.28 nM, respectively) at the human A3AR. These compounds showed anti-growth effects on HL-60 leukemia cell, which resulted from the inhibition of Wnt signaling pathway. Copyright © Taylor & Francis Group, LLC.
DOI
10.1080/15257770701547107
Appears in Collections:
약학대학 > 약학과 > Journal papers
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