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Design, synthesis, and biological activity of N6-substituted-4′-thioadenosines at the human A3 adenosine receptor

Title
Design, synthesis, and biological activity of N6-substituted-4′-thioadenosines at the human A3 adenosine receptor
Authors
Jeong L.S.Lee H.W.Kim H.O.Jung J.Y.Gao Z.-G.Duong H.T.Rao S.Jacobson K.A.Shin D.H.Lee J.A.Gunaga P.Lee S.K.Jin D.Z.Chun M.W.Moon H.R.
Ewha Authors
정낙신이상국
Issue Date
2006
Journal Title
Bioorganic and Medicinal Chemistry
ISSN
0968-0896JCR Link
Citation
vol. 14, no. 14, pp. 4718 - 4730
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
A large series of N6-substituted-4′-thioadenosines were synthesized starting from d-gulonic-γ-lactone, and structure-activity relationships were studied at the human A3 and other subtypes of adenosine receptors (ARs). 2-Chloro-substituted and 2-H analogues were compared. 2-Chloro-N6-methyl-4′-thioadenosine 19b was a highly potent and selective agonist (Ki = 0.8 ± 0.1 nM in binding) at the A3AR, and displayed the same relative efficacy in receptor activation as a known full agonist, Cl-IB-MECA. Most of N6-substituted-4′-thioadenosines were less potent in binding than the corresponding N6-substituted-adenosines or N6-substituted-4′-thioadenosine-5′-uronamides. N6-(3-Iodobenzyl) derivative 19g was demonstrated to be an A3AR-selective partial agonist displaying a Ki value of 3.2 nM. © 2006 Elsevier Ltd. All rights reserved.
DOI
10.1016/j.bmc.2006.03.030
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약학대학 > 약학과 > Journal papers
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