title: 2-Phenylquinolones as inhibitors of the HIV-1 Tat-TAR interaction.
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.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università di Padova, Via Marzolo 5, 35131 Padova, Italy. barbara.gatto@unipd.it
authors.forename: Barbara
authors.initials: B
authors.lastname: Gatto
authors.forename: Oriana
authors.initials: O
authors.lastname: Tabarrini
authors.forename: Serena
authors.initials: S
authors.lastname: Massari
authors.forename: Giulia
authors.initials: G
authors.lastname: Giaretta
authors.forename: Stefano
authors.initials: S
authors.lastname: Sabatini
authors.forename: Claudia
authors.initials: C
authors.lastname: Del Vecchio
authors.forename: Cristina
authors.initials: C
authors.lastname: Parolin
authors.forename: Arnaldo
authors.initials: A
authors.lastname: Fravolini
authors.forename: Manlio
authors.initials: M
authors.lastname: Palumbo
authors.forename: Violetta
authors.initials: V
authors.lastname: Cecchetti
mesh_terms: D000595:Amino Acid Sequence; D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D002460:Cell Line; D016325:HIV Long Terminal Repeat / Q000187:drug effects*; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans; D019169:Jurkat Cells; D008969:Molecular Sequence Data; D011485:Protein Binding; D015363:Quinolones / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D013329:Structure-Activity Relationship; D054322:tat Gene Products, Human Immunodeficiency Virus / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D019380:Anti-HIV Agents; D015363:Quinolones; D054322:tat Gene Products, Human Immunodeficiency Virus