First Synthesis and Anti-HIV Evaluation of 4′-Methyl-Cyclopentanyl 9-Deazaadenosine |
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| Authors: | Chang Hyun Oh Lian Jin Liu Joon Hee Hong |
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| Institution: | 1. Medicinal Chemistry Research Center , Korea Institute of Science and Technology , Seoul , Republic of Korea;2. BK21-Project Team, College of Pharmacy , Chosun University , Kwangju , Republic of Korea |
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| Abstract: | The first synthesis of a 4′-methylated carbocyclic C-nucleoside 16 was achieved via the mesylate intermediate 10, which was prepared using ring-closing metathesis and SN2 alkylation from acetol 5. When antiviral evaluation of synthesized compound 16 was performed against various viruses such as HIV, HSV-1, HSV-2, and HCMV, it showed moderate anti-HIV activity in MT-4 cell line (EC50 = 14.7 μmol). |
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| Keywords: | Carbocyclic C-nucleoside antiviral agents SN2 alkylation |
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