title: Design, synthesis, and biological evaluation of novel quinoline derivatives as HIV-1 Tat-TAR interaction inhibitors.
abstract: 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.
authors.affiliation: State Key Laboratory of Natural and Biomimetic Drugs, Peking University, Beijing, China.
authors.forename: Shuguang
authors.initials: S
authors.lastname: Chen
authors.forename: Ran
authors.initials: R
authors.lastname: Chen
authors.forename: Meizi
authors.initials: M
authors.lastname: He
authors.forename: Ruifang
authors.initials: R
authors.lastname: Pang
authors.forename: Zhiwu
authors.initials: Z
authors.lastname: Tan
authors.forename: Ming
authors.initials: M
authors.lastname: Yang
mesh_terms: D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D015195:Drug Design; D016325:HIV Long Terminal Repeat / Q000187:drug effects*; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans; D011804:Quinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D054322:tat Gene Products, Human Immunodeficiency Virus / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D019380:Anti-HIV Agents; D011804:Quinolines; D054322:tat Gene Products, Human Immunodeficiency Virus