2-Phenylquinolones as inhibitors of the HIV-1 Tat-TAR interaction.
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.
Gatto
Barbara
B
Dipartimento di Scienze Farmaceutiche, Università di Padova, Via Marzolo 5, 35131 Padova, Italy. barbara.gatto@unipd.it
Tabarrini
Oriana
O
Massari
Serena
S
Giaretta
Giulia
G
Sabatini
Stefano
S
Del Vecchio
Claudia
C
Parolin
Cristina
C
Fravolini
Arnaldo
A
Palumbo
Manlio
M
Cecchetti
Violetta
V
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
D019380:Anti-HIV Agents; D015363:Quinolones; D054322:tat Gene Products, Human Immunodeficiency Virus