| Literature DB >> 19072694 |
Hyo-Joong Kim1, Ashoke Sharon, Chandralata Bal, Jianing Wang, Madhan Allu, Zhuhui Huang, Michael G Murray, Leda Bassit, Raymond F Schinazi, Brent Korba, Chung K Chu.
Abstract
A series of 7-deazaneplanocin A (7-DNPA, 2) analogues were synthesized and evaluated for in vitro antiviral activity against HBV and HCV. The syntheses of target carbocyclic nucleosides were accomplished via a convergent procedure. 7-Substitutions were introduced by using 7-substituted-7-deaza heterocyclic base precursors (F, Cl, Br, and I) or via substitution reactions after the synthesis of the carbocyclic nucleosides. Among the synthesized compounds, 2, 13-15, 24, and 27 exhibited significant anti-HCV activity (EC(50) ranged from 1.8 to 20.1 microM) and compounds 2, 15, 22, and 24 demonstrated moderate to potent anti-HBV activity (EC(50) = 0.3-3.3 microM). In addition, compound 24 also showed activity against lamivudine- and adefovir-associated HBV mutants.Entities:
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Year: 2009 PMID： 19072694 PMCID： PMC2725430 DOI： 10.1021/jm801418v
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446