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N6-substituted D-4′-thioadenosine-5′-methyluronamides: Potent and selective agonists at the human A3 adenosine receptor

Title
N6-substituted D-4′-thioadenosine-5′-methyluronamides: Potent and selective agonists at the human A3 adenosine receptor
Authors
Jeong L.S.Jin D.Z.Kim H.O.Shin D.H.Moon H.R.Gunaga P.Chun M.W.Kim Y.-C.Melman N.Gao Z.-G.Jacobson K.A.
Ewha Authors
정낙신
Issue Date
2003
Journal Title
Journal of Medicinal Chemistry
ISSN
0022-2623JCR Link
Citation
vol. 46, no. 18, pp. 3775 - 3777
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
4′-Thio analogues 3-5 of Cl-IB-MECA (2) (Ki = 1.0 ± 0.2 nM at the human A3 adenosine receptor) were synthesized from D-gulono-γ-lactone via 4-thioribosyl acetate 14 as the key intermediate. All synthesized 4′-thionucleosides exhibited higher binding affinity to the human A3 adenosine receptor than Cl-IB-MECA, among which 4 showed the most potent binding affinity (Ki = 0.28 ± 0.09 nM). 4 was also selective for A3 vs human A1 and human A2A receptors by 4800- and 36000-fold, respectively.
DOI
10.1021/jm034098e
Appears in Collections:
약학대학 > 약학과 > Journal papers
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