Synthesis of 2-alkynyl substituted 4′-thioadenosine derivatives and their binding affinities at the adenosine receptors

被引：0
作者：
Cheng-Wu Liang
Won Jun Choi
Lak Shin Jeong
机构：
[1] Ewha Womans University,Laboratory of Medicinal Chemistry, College of Pharmacy
[2] Jilin Medical College,College of Pharmacy
来源：
Archives of Pharmacal Research | 2008年 / 31卷
关键词：
2-Alkynyl-substituted-; -methyl-4′-thioadenosine; A; adenosine receptor; Palladium-catalyzed cross coupling; Binding affinity; Diazotization;
D O I：
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摘要：
On the basis of high binding affinity of 2-hexynyl-N6-methyladenosine and N6-substituted-4′-thioadenosine derivatives at the A3 adenosine receptor (AR), novel 2-alkynyl-substituted-N6-methyl-4′-thioadenosine derivatives, combining the characteristics of two classes of nucleosides were designed and synthesized from D-gulonic γ-lactone via palladium-catalyzed cross coupling reaction as a key step. Among compounds tested, only compound 3b showed moderate binding affinity at the human A3 adenosine receptor without binding affinities at other subtypes.
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