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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:
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.
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页码:935 / 938
页数:4
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