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Design, synthesis, and biological evaluation of novel quinoline derivatives as HIV-1 Tat-TAR interaction inhibitors. 2009

Shuguang Chen, and Ran Chen, and Meizi He, and Ruifang Pang, and Zhiwu Tan, and Ming Yang
State Key Laboratory of Natural and Biomimetic Drugs, Peking University, Beijing, China.

Thirty-two quinoline derivatives were designed and synthesized as HIV-1 Tat-TAR interaction inhibitors. All the compounds showed high antiviral activities in inhibiting the formation of SIV-induced syncytium in CEM174 cells. Nine of them with low cytotoxicities were evaluated by Tat dependent HIV-1 LTR-driven CAT gene expression colorimetric enzyme assay in human 293T cells, indicating effective inhibitory activities of blocking the Tat-TAR interaction. Molecular modeling experiments indicated that these compounds may inhibit Tat-TAR interaction by binding to Tat protein instead of TAR RNA.

UI MeSH Term Description Entries
D011804 Quinolines
D002460 Cell Line Established cell cultures that have the potential to propagate indefinitely. Cell Lines,Line, Cell,Lines, Cell
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D013329 Structure-Activity Relationship The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups. Relationship, Structure-Activity,Relationships, Structure-Activity,Structure Activity Relationship,Structure-Activity Relationships
D015195 Drug Design The molecular designing of drugs for specific purposes (such as DNA-binding, enzyme inhibition, anti-cancer efficacy, etc.) based on knowledge of molecular properties such as activity of functional groups, molecular geometry, and electronic structure, and also on information cataloged on analogous molecules. Drug design is generally computer-assisted molecular modeling and does not include PHARMACOKINETICS, dosage analysis, or drug administration analysis. Computer-Aided Drug Design,Computerized Drug Design,Drug Modeling,Pharmaceutical Design,Computer Aided Drug Design,Computer-Aided Drug Designs,Computerized Drug Designs,Design, Pharmaceutical,Drug Design, Computer-Aided,Drug Design, Computerized,Drug Designs,Drug Modelings,Pharmaceutical Designs
D015497 HIV-1 The type species of LENTIVIRUS and the etiologic agent of AIDS. It is characterized by its cytopathic effect and affinity for the T4-lymphocyte. Human immunodeficiency virus 1,HIV-I,Human Immunodeficiency Virus Type 1,Immunodeficiency Virus Type 1, Human
D016325 HIV Long Terminal Repeat Regulatory sequences important for viral replication that are located on each end of the HIV genome. The LTR includes the HIV ENHANCER, promoter, and other sequences. Specific regions in the LTR include the negative regulatory element (NRE), NF-kappa B binding sites , Sp1 binding sites, TATA BOX, and trans-acting responsive element (TAR). The binding of both cellular and viral proteins to these regions regulates HIV transcription. HIV Negative Regulatory Element,HIV Sp1-Binding Site,HIV Trans-Acting Responsive Region,Human Immunodeficiency Virus Long Terminal Repeat,Long Terminal Repeat, HIV,Negative Regulatory Element, HIV,Sp1-Binding Site, HIV,Trans-Acting Responsive Region, HIV,HIV-1 LTR,Human Immunodeficiency Virus LTR,LTR, Human Immunodeficiency Virus,TAR Element, HIV,Trans-Activation Responsive Element, HIV,Trans-Activation Responsive Region, HIV,HIV 1 LTR,HIV Sp1 Binding Site,HIV Sp1-Binding Sites,HIV TAR Element,HIV TAR Elements,HIV Trans Acting Responsive Region,LTR, HIV-1,Sp1 Binding Site, HIV,Sp1-Binding Sites, HIV,TAR Elements, HIV,Trans Acting Responsive Region, HIV,Trans Activation Responsive Element, HIV,Trans Activation Responsive Region, HIV
D054322 tat Gene Products, Human Immunodeficiency Virus Proteins encoded by the TAT GENES of the HUMAN IMMUNODEFICIENCY VIRUS. HIV Transacting Transcription Protein,HIV tat Protein,Trans-Acting Transcription Factor, HIV,Trans Acting Transcription Factor, HIV,tat Protein, HIV
D019380 Anti-HIV Agents Agents used to treat AIDS and/or stop the spread of the HIV infection. These do not include drugs used to treat symptoms or opportunistic infections associated with AIDS. AIDS Drug,AIDS Drugs,Anti-AIDS Agents,Anti-AIDS Drug,Anti-HIV Agent,Anti-HIV Drug,Anti-AIDS Drugs,Anti-HIV Drugs,Agent, Anti-HIV,Agents, Anti-AIDS,Agents, Anti-HIV,Anti AIDS Agents,Anti AIDS Drug,Anti AIDS Drugs,Anti HIV Agent,Anti HIV Agents,Anti HIV Drug,Anti HIV Drugs,Drug, AIDS,Drug, Anti-AIDS,Drug, Anti-HIV,Drugs, AIDS,Drugs, Anti-AIDS,Drugs, Anti-HIV

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