Structure-guided design of A3 adenosine receptor-selective nucleosides: combination of 2-arylethynyl and bicyclo [3.1. 0] hexane substitutions

…, TC Wan, E Gizewski, JA Auchampach…

文献索引：Tosh, Dilip K.; Deflorian, Francesca; Phan, Khai; Gao, Zhan-Guo; Wan, Tina C.; Gizewski, Elizabeth; Auchampach, John A.; Jacobson, Kenneth A. Journal of Medicinal Chemistry, 2012 , vol. 55, # 10 p. 4847 - 4860

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被引用次数: 38

摘要

(N)-Methanocarba adenosine 5′-methyluronamides containing known A3 AR (adenosine receptor)-enhancing modifications, ie, 2-(arylethynyl) adenine and N 6-methyl or N 6-(3- substituted-benzyl), were nanomolar full agonists of human (h) A3AR and highly selective (K i∼ 0.6 nM, N 6-methyl 2-(halophenylethynyl) analogues 13 and 14). Combined 2- arylethynyl-N 6-3-chlorobenzyl substitutions preserved A3AR affinity/selectivity in the (N)- ...