2. Academic Validation
  3. Synthesis and anti-hepatitis C virus (HCV) activity of 3'-C-substituted-methyl pyrimidine and purine nucleosides

Synthesis and anti-hepatitis C virus (HCV) activity of 3'-C-substituted-methyl pyrimidine and purine nucleosides

  • Bioorg Med Chem. 2010 Jul 1;18(13):4812-20. doi: 10.1016/j.bmc.2010.05.002.
Won Jun Choi 1,  Yu Min Kim,  Hea Ok Kim,  Hyuk Woo Lee,  Dong-Eun Kim,  Kwang-su Park,  Youhoon Chong,  Lak Shin Jeong
Affiliations

Affiliation

  • 1 Department of Bioinspired Science, Ewha Womans University, 11-1 Seodaemun-gu, Daehyun-dong, Seoul 120-750, Republic of Korea.
PMID: 20627592 DOI: 10.1016/j.bmc.2010.05.002
Abstract

On the basis of potent anti-hepatitis C virus (HCV) activity of 2'-C-hydroxymethyladenosine, 3'-C-substituted-methyl-ribofuranosyl pyrimidine and purine nucleosides were designed and synthesized from D-xylose. Among compounds tested, all adenine analogues, 4a, 4d, and 4g showed significant anti-HCV activity in a replicon-based cell assay irrespective of the substituent (Y=OH, N₃, or F) at the 3'-C-substituted methyl position, among which 4g (Y=N₃) was the most potent, but it is also cytotoxic. This study guarantees the 3'-C-substituted-methyl nucleoside serves as a new template for the development of new anti-HCV agents.

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