Cytostatic 6-arylpurine nucleosides. 6. SAR in anti-HCV and cytostatic activity of extended series of 6-hetarylpurine ribonucleosides
Cytostatic 6-arylpurine nucleosides. 6. SAR in anti-HCV and cytostatic activity of extended series of 6-hetarylpurine ribonucleosides
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DOI：
10.1021/jm050335x
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发表时间：
2005-09-08
影响因子：
7.3
通讯作者：
Otto, MJ
中科院分区：
文献类型：
--
作者：
Hocek, M;Naus, P;Otto, MJ
6-杂芳基嘌呤核糖核苷的显着抗 HCV 活性已被发现并在此首次报道，并与细胞抑制作用进行了比较。通过嘌呤核苷 6 位的杂环化或通过 6-氯嘌呤核苷与杂芳基硼酸、-锡烷或-卤化锌的交叉偶联，制备了一系列扩展的 6-杂芳基嘌呤核糖核苷。最具抗HCV活性的是带有吡咯-3-基(3k)或2-呋喃基(3g)基团的嘌呤核糖核苷，分别发挥EC90＝0.14和0.4μM。
Significant anti-HCV activity of 6-hetarylpurine ribonucleosides has been discovered and is reported here for the first time and compared with cytostatic effect. An extended series of 6-hetarylpurine ribonucleosides has been prepared by heterocyclizations in position 6 of purine nucleosides or by cross-couplings of 6-chloropurine nucleosides with hetarylboronic acids, -stannanes, or -zinc halides. The most anti-HCV active were purine ribonucleosides bearing pyrrol-3-yl (3k) or 2-furyl (3g) groups exerting EC90 = 0.14 and 0.4 mu M, respectively.