Communication

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

  1. Barbara Gatto Prof.1,
  2. Oriana Tabarrini Prof.2,
  3. Serena Massari Dr.2,
  4. Giulia Giaretta Dr.1,
  5. Stefano Sabatini Dr.2,
  6. Claudia Del Vecchio Dr.3,
  7. Cristina Parolin Prof.4,
  8. Arnaldo Fravolini Prof.2,
  9. Manlio Palumbo Prof.1,
  10. Violetta Cecchetti Prof.2

Article first published online: 12 MAR 2009

DOI: 10.1002/cmdc.200800437

Issue

ChemMedChem

ChemMedChem

Special Issue: XIX NMMC Verona 2008

Volume 4, Issue 6, pages 935–938, June 8, 2009

Additional Information

How to Cite

Gatto, B., Tabarrini, O., Massari, S., Giaretta, G., Sabatini, S., Del Vecchio, C., Parolin, C., Fravolini, A., Palumbo, M. and Cecchetti, V. (2009), 2-Phenylquinolones as Inhibitors of the HIV-1 Tat–TAR Interaction. ChemMedChem, 4: 935–938. doi: 10.1002/cmdc.200800437

Author Information

  1. 1

    Dipartimento di Scienze Farmaceutiche, Università di Padova, Via Marzolo 5, 35131 Padova (Italy), Fax: (+39) 049-827-5366

  2. 2

    Dipartimento di Chimica e Tecnologia del Farmaco, Università di Perugia, Via del Liceo 1, 06123 Perugia (Italy), Fax: (+39) 075-585-5115

  3. 3

    Dipartimento di Istologia, Microbiologia e Biotecnologie Mediche, Università di Padova, Via Gabelli 63, 35121 Padova (Italy)

  4. 4

    Dipartimento di Biologia, Università di Padova, Via Ugo Bassi 58/B, 35131 Padova (Italy)

Publication History

  1. Issue published online: 28 MAY 2009
  2. Article first published online: 12 MAR 2009
  3. Manuscript Revised: 15 JAN 2009
  4. Manuscript Received: 15 DEC 2008

Funded by

  • MIUR

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Keywords:

  • 2-phenylquinolones;
  • antiviral agents;
  • fluorescence quenching assay;
  • medicinal chemistry;
  • Tat–TAR inhibitors

Abstract

Thumbnail image of graphical 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.

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