Abstract
The synthesis and antiviral evaluation of unsymmetrical indolocarbazole derivatives of Arcyriaflavin A, substituted with a range of alkyl groups at the indole nitrogen, is described. Structure-activity relationships in this series against human cytomegalovirus (HCMV) replication in cell culture are reported. Compound 4b was identified as potent inhibitor of HCMV (IC(50)=19 nM), which retained activity against a range of HCMV strains including ganciclovir resistant isolates.
MeSH terms
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Antiviral Agents / chemical synthesis*
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Antiviral Agents / pharmacology*
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Carbazoles / chemical synthesis
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Carbazoles / pharmacology*
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Cells, Cultured
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Cytomegalovirus / drug effects*
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Drug Resistance / genetics
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Drug Resistance / physiology
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Ganciclovir / pharmacology
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Humans
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Indoles / chemical synthesis
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Indoles / pharmacology*
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Inhibitory Concentration 50
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Protein Kinase C / antagonists & inhibitors
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Structure-Activity Relationship
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Virus Replication / drug effects*
Substances
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Antiviral Agents
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Carbazoles
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Indoles
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arcyriaflavin A
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Protein Kinase C
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Ganciclovir