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Design, synthesis, and binding of homologated truncated 4′-thioadenosine derivatives at the human A3 adenosine receptors

Title
Design, synthesis, and binding of homologated truncated 4′-thioadenosine derivatives at the human A3 adenosine receptors
Authors
Lee H.W.Kim H.O.Choi W.J.Choi S.Lee J.H.Park S.-G.Yoo L.Jacobson K.A.Jeong L.S.
Ewha Authors
정낙신최선최원준
SCOPUS Author ID
최선scopus
Issue Date
2010
Journal Title
Bioorganic and Medicinal Chemistry
ISSN
0968-0896JCR Link
Citation
vol. 18, no. 19, pp. 7015 - 7021
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
We synthesized homologated truncated 4′-thioadenosine analogues 3 in which a methylene (CH2) group was inserted in place of the glycosidic bond of a potent and selective A3 adenosine receptor antagonist 2. The analogues were designed to induce maximum binding interaction in the binding site of the A3 adenosine receptor. However, all homologated nucleosides were devoid of binding affinity at all subtypes of adenosine receptors, indicating that free rotation through the single bond allowed the compound to adopt an indefinite number of conformations, disrupting the favorable binding interaction essential for receptor recognition. © 2010 Elsevier Ltd. All rights reserved.
DOI
10.1016/j.bmc.2010.08.018
Appears in Collections:
약학대학 > 약학과 > Journal papers
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