Abstract
Novel L- and D-configuration dioxolane 5-azacytosine and 6-azathymine nucleosides have been synthesized and evaluated for biological activity. (-)-(2S,4S)-1-[2-(Hydroxymethyl)-1,3-dioxolan-4-yl]-5-azacytosine (6) showed significant activity against HBV, whereas the D-configuration analogue (14) has been found to exhibit potent anti-HIV activity.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Anti-HIV Agents / chemical synthesis
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Anti-HIV Agents / pharmacology
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / pharmacology
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Antiviral Agents / chemical synthesis
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Antiviral Agents / pharmacology
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Cell Division / drug effects
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Cytosine / analogs & derivatives*
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Cytosine / chemical synthesis
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Cytosine / pharmacology
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Dioxolanes / chemical synthesis
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Dioxolanes / pharmacology
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HIV-1 / drug effects
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Hepatitis B virus / drug effects
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Herpesvirus 1, Human / drug effects
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Herpesvirus 2, Human / drug effects
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Humans
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Inhibitory Concentration 50
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Magnetic Resonance Spectroscopy
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Nucleosides / chemical synthesis*
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Nucleosides / pharmacology*
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Structure-Activity Relationship
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Thymine / analogs & derivatives*
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Thymine / chemical synthesis
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Thymine / pharmacology
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Tumor Cells, Cultured / drug effects
Substances
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Anti-HIV Agents
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Antineoplastic Agents
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Antiviral Agents
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Dioxolanes
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Nucleosides
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5-azacytosine
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Cytosine
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Thymine
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formal glycol
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6-azathymine