Abstract
Sixteen novel compounds; 3alpha-methoxyserrat-14-en-21beta-ol (1) and 3beta-methoxyserrat-14-en-21beta-ol (2) and their curcumin, kojic acid, quercetin, and baicalein conjugates (3)-(18) were designed, synthesized, and evaluated for in vitro anti-HIV-1 reverse transcriptase (RT) activity in infected C8166-CCR5 cells, a human CD4(+) T-lymphocyte cell line. Among them, kojic acid derivatives, 9-12 showed significant biological activity. In particular, the compound 13, the conjugate of two molecules of 3alpha-methoxyserrat-14-en-21beta-ol (1) and one molecule of kojic acid, exerted significant anti-HIV activity with an EC50 value of 0.12microg/mL.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antiviral Agents / chemical synthesis
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Antiviral Agents / chemistry*
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Antiviral Agents / pharmacology*
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Cell Line
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Cell Survival / drug effects
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Curcumin / chemical synthesis
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Curcumin / chemistry
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Curcumin / pharmacology
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Flavanones / chemical synthesis
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Flavanones / chemistry
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Flavanones / pharmacology
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HIV Infections / drug therapy*
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HIV-1 / drug effects
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HIV-1 / enzymology*
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Humans
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Molecular Structure
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Pyrones / chemical synthesis
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Pyrones / chemistry
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Pyrones / pharmacology
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Quercetin / chemical synthesis
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Quercetin / chemistry
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Quercetin / pharmacology
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RNA-Directed DNA Polymerase / metabolism
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Reverse Transcriptase Inhibitors / chemical synthesis
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Reverse Transcriptase Inhibitors / chemistry
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Reverse Transcriptase Inhibitors / pharmacology
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T-Lymphocytes / drug effects
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T-Lymphocytes / virology
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Triterpenes / chemical synthesis
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Triterpenes / chemistry*
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Triterpenes / pharmacology*
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Viral Proteins / antagonists & inhibitors
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Viral Proteins / metabolism
Substances
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3beta-methoxyserrat-14-en-21beta-ol
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Antiviral Agents
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Flavanones
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Pyrones
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Reverse Transcriptase Inhibitors
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Triterpenes
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Viral Proteins
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baicalein
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kojic acid
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Quercetin
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RNA-Directed DNA Polymerase
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Curcumin