Synthesis and general biological activity of a small adenosine-5'-(carboxamide and sulfanilamide) library.
Synthesis and general biological activity of a small adenosine-5'-(carboxamide and sulfanilamide) library.
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小型腺苷-5-（羧酰胺和磺胺）文库的合成和一般生物活性。
DOI：
10.1080/15257770.2014.931588
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发表时间：
2014
期刊：
影响因子：
--
通讯作者：
Reynolds,RobertC
中科院分区：
文献类型：
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作者：
Moukha-Chafiq,Omar;Reynolds,RobertC
在NIH路线图倡议的中试规模文库（PSL）计划下，从2′，3 ′-O-异亚丙基腺苷-5 ′-羧酸2合成了55个腺苷肽类似物的小文库。胺或磺胺反应物与2的游离5′-羧酸部分以自动化溶液相方式偶联，在酸介导的水解后以良好的产率和高纯度得到目标化合物3 - 57。在初步的细胞检测中没有发现明显的抗癌或抗疟疾活性。然而，通过MLPCN程序的初步筛选表明，这些类似物可能显示出不同的和有趣的生物活性。
A small library of fifty-five adenosine peptide analogs was synthesized, under the Pilot Scale Library (PSL) Program of the NIH Roadmap initiative, from 2′,3′-O-isopropylideneadenosine-5′-carboxylic acid2. The coupling of amine or sulfanilamide reactants to the free 5′-carboxylic acid moiety of2, in automated solution-phase fashion, led after acid-mediated hydrolysis to target compounds3–57in good yields and high purity. No marked anticancer or antimalarial activity was noted on preliminary cellular testing. Initial screening through the MLPCN program, however, indicates that these analogs may show diverse and interesting biological activities.