In:
Molecules, MDPI AG, Vol. 27, No. 7 ( 2022-03-31), p. 2283-
Abstract:
The adenosine A3 receptor is a promising target for treating and diagnosing inflammation and cancer. In this paper, a series of bicyclo[3.1.0]hexane-based nucleosides was synthesized and evaluated for their P1 receptor affinities in radioligand binding studies. The study focused on modifications at 1-, 2-, and 6-positions of the purine ring and variations of the 5′-position at the bicyclo[3.1.0] hexane moiety, closing existing gaps in the structure–affinity relationships. The most potent derivative 30 displayed moderate A3AR affinity (Ki of 0.38 μM) and high A3R selectivity. A subset of compounds varied at 5′-position was further evaluated in functional P2Y1R assays, displaying no off-target activity.
Type of Medium:
Online Resource
ISSN:
1420-3049
DOI:
10.3390/molecules27072283
Language:
English
Publisher:
MDPI AG
Publication Date:
2022
detail.hit.zdb_id:
2008644-1
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