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Cancer Ther. 2004, 3, 1375). More recently, SAR studies of the 4-aryl-4H-chromenes revealed that disubstitution at the 7,8-positions were preferred over 5,6 or 6,7-positions (Kemnitzer, W. et al. Bioorg. Med. Chem. Lett. 2005, 15, 4745). Additional SAR studies involving a fused ring at the 7, 8-positions resulted in potent analogs. Herein we will report in detail the chemistry, in vitro and in vivo characterization of compounds with a N-substituted pyrrole fused ring at the 7, 8positions. 2]octane-3-ol Abeer M Al-Ghananeem1, Zaineb Al-Beyati1, Ahmad H Malkawi1, Vijayakumar N Sonar1, Michael Freeman2, and Peter A.
In seeking ways to circumvent this, our attention was drawn to 5'-noraristeromycin (2) that is a derivative of the carbocyclic nucleoside aristeromyin (3) with antiviral properties yet is devoid of the toxicity of aristeromycin, also a property of nucleotide formation. This report describes a combination of the structural components of 1 and 2 resulting in carbocyclic 5'-norformycin (4). This research was supported by funds from the Department of Health and Human Services (AI 56540). MEDI 82 Synthesis and the antiviral activity of 3-methyl-3-deaza-5'noraristeromycin Chong Liu and Stewart W.
Nucleosides based on this scaffold were originally introduced to investigate the conformational preferences of kinases and polymerases. However, some conformationally restricted nucleosides also showed interesting antiviral properties. Among these, N-MCT was found to exhibit greater antiherpetic activity against herpes virus types 1 (HSV-1), 2 (HSV-2) and Kaposi's sarcoma-associated herpesvirus (KSHV) than the reference compounds acyclovir and gancyclovir. In our search for a convenient and economic route for the large scale synthesis of N-MCT, we decided to investigate different strategies for introducing the heterocyclic base into the carbocyclic moiety.