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Design, synthesis, and anti-tumor activity of 4′-thionucleosides as potent and selective agonists at the human A3 adenosine receptor
- Design, synthesis, and anti-tumor activity of 4′-thionucleosides as potent and selective agonists at the human A3 adenosine receptor
- 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
- 정낙신; 이상국
- Issue Date
- Journal Title
- Nucleosides, Nucleotides and Nucleic Acids
- vol. 26, no. 41559, pp. 1565 - 1568
- SCIE; SCOPUS
- 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.
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- 약학대학 > 약학과 > Journal papers
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