Abstract
A novel compound inhibiting HIV-1 integrase has been identified by means of virtual screening techniques. A small family of structurally related molecules has been synthesized and biologically evaluated with some of the compounds possessing micromolar activity both in enzymatic and cellular assays.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Anti-HIV Agents / chemical synthesis
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Anti-HIV Agents / chemistry*
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Anti-HIV Agents / pharmacology
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Cell Line
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HIV Integrase / chemistry*
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HIV Integrase / metabolism
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HIV Integrase Inhibitors / chemical synthesis
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HIV Integrase Inhibitors / chemistry*
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HIV Integrase Inhibitors / pharmacology
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HIV-1 / drug effects*
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Humans
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Rhodanine / chemical synthesis
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Rhodanine / chemistry*
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Structure-Activity Relationship
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Thiobarbiturates / chemical synthesis
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Thiobarbiturates / chemistry*
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Thiohydantoins / chemical synthesis
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Thiohydantoins / chemistry*
Substances
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Anti-HIV Agents
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HIV Integrase Inhibitors
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Thiobarbiturates
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Thiohydantoins
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Rhodanine
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HIV Integrase
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thiobarbituric acid
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p31 integrase protein, Human immunodeficiency virus 1