Cytostatic 6-arylpurine nucleosides III.: Synthesis and structure-activity relationship study in cytostatic activity of 6-aryl-, 6-hetaryl- and 6-benzylpurine ribonucleosides
Cytostatic 6-arylpurine nucleosides III.: Synthesis and structure-activity relationship study in cytostatic activity of 6-aryl-, 6-hetaryl- and 6-benzylpurine ribonucleosides
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DOI：
10.1135/cccc20010483
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发表时间：
2001-03-01
影响因子：
--
通讯作者：
Dvorákova, H
中科院分区：
文献类型：
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作者：
Hocek, M;Holy, A;Dvorákova, H
6-氯-9-（2，3，5-三-O-乙酰基-β-D-呋喃核糖基）-嘌呤与芳基硼酸、杂芳基卤化锌、杂芳基锡烷或苄基卤化锌在钯催化下发生交叉偶联反应，然后脱保护，合成了15个6-芳基、6-杂芳基和6-苄基嘌呤核苷。构效关系研究表明，除了6-（4-取代苯基）嘌呤核苷外，一些6-杂芳基和6-苄基嘌呤核苷也具有相当的细胞抑制活性。
A series of fifteen 6-aryl-, 6-hetaryl- and 6-benzylpurine ribonucleosides has been prepared by Pd-catalyzed cross-coupling reactions of 6-chloro-9-(2,3,5-tri-O-acetyl-beta -D-ribofuranosyl)-purine with arylboronic acids, hetarylzinc halides, hetarylstannanes or benzylzinc halides followed by deprotection. Structure-activity relationship study revealed that besides 6-(4-substituted phenyl)purine nucleosides, also some 6-hetaryl- and 6-benzylpurine ribonucleosides possess considerable cytostatic activity.