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

✍ Scribed by Barbara Gatto; Oriana Tabarrini; Serena Massari; Giulia Giaretta; Stefano Sabatini; Claudia Del Vecchio; Cristina Parolin; Arnaldo Fravolini; Manlio Palumbo; Violetta Cecchetti

Publisher
John Wiley and Sons
Year
2009
Tongue
English
Weight
202 KB
Volume
4
Category
Article
ISSN
1860-7179

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✦ Synopsis

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.magnified image

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✍ Steffen Renner; Verena Ludwig; Oliver Boden; Ute Scheffer; Michael Göbel; Gisber 📂 Article 📅 2005 🏛 John Wiley and Sons 🌐 English ⚖ 399 KB

## Abstract __TAR RNA is a potential target for AIDS therapy. Ligand‐based virtual screening was performed to retrieve novel scaffolds for RNA‐binding molecules capable of inhibiting the Tat–TAR interaction, which is essential for HIV replication. We used a “fuzzy” pharmacophore approach (SQUID) an