Cytostatic 6-Arylpurine Nucleosides. 6. SAR in Anti-HCV and Cytostatic Activity of Extended Series of 6-Hetarylpurine Ribonucleosides
Journal of Medicinal Chemistry2005Vol. 48(18), pp. 5869–5873
Citations Over TimeTop 10% of 2005 papers
Michal Hocek, Petr Nauš, Radek Pohl, Ivan Votruba, Phillip A. Furman, Phillip M. Tharnish, Michaël Otto
Abstract
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 nucleosides 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 or 2-furyl groups exerting EC(90) = 0.14 and 0.4 microM, respectively.
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