2-Phenylquinolones as Inhibitors of the HIV-1 Tat-TAR Interaction

被引：18

作者：

Gatto, Barbara ^{[1
]}

Tabarrini, Oriana ^{[2
]}

Massari, Serena ^{[2
]}

Giaretta, Giulia ^{[1
]}

Sabatini, Stefano ^{[2
]}

Del Vecchio, Claudia ^{[3
]}

Parolin, Cristina ^{[4
]}

Fravolini, Arnaldo ^{[2
]}

Palumbo, Manlio ^{[1
]}

Cecchetti, Violetta ^{[2
]}

机构：

[1] Univ Padua, Dipartimento Sci Farmaceut, I-35131 Padua, Italy

[2] Univ Perugia, Dipartimento Chim & Tecnol Farmaco, I-06123 Perugia, Italy

[3] Univ Padua, Dipartimento Istol Microbiol & Biotecnol Med, I-35121 Padua, Italy

[4] Univ Padua, Dipartimento Biol, I-35131 Padua, Italy

来源：

CHEMMEDCHEM | 2009年 / 4卷 / 06期

关键词：

2-phenylquinolones; antiviral agents; fluorescence quenching assay; medicinal chemistry; Tat-TAR inhibitors; BIOLOGICAL EVALUATION; RNA; BINDING; PROTEIN; DESIGN;

D O I：

10.1002/cmdc.200800437

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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. (Chemical Equation Presented) © 2009 Wiley-VCH Verlag GmbH& Co. KGaA.

引用

页码：935 / 938

页数：4

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