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
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
收藏
页码:935 / 938
页数:4
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