Abstract
Novel 2-phenylquinolones aimed at the Tat-TAR complex were synthesized and tested. Derivatives characterized by precise modifications of the quinolone nucleus and to the side chain of the 2-phenyl ring allowed a thorough structure-activity study, confirming 2-phenylquinolone as a suitable scaffold for inhibition of the Tat-TAR interaction.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Amino Acid Sequence
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Anti-HIV Agents / chemical synthesis
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Anti-HIV Agents / chemistry*
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Anti-HIV Agents / toxicity
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Cell Line
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HIV Long Terminal Repeat / drug effects*
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HIV-1 / drug effects*
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Humans
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Jurkat Cells
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Molecular Sequence Data
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Protein Binding
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Quinolones / chemical synthesis
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Quinolones / chemistry*
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Quinolones / toxicity
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Structure-Activity Relationship
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tat Gene Products, Human Immunodeficiency Virus / antagonists & inhibitors*
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tat Gene Products, Human Immunodeficiency Virus / metabolism
Substances
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Anti-HIV Agents
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Quinolones
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tat Gene Products, Human Immunodeficiency Virus