We have synthesized an extended series of 2-PQs, tested their activity on the Tat–TAR complex, and obtained novel compounds that exhibit higher activity while expanding our structure–activity analysis study for this new class of inhibitors. Our results demonstrate that the achievement of in vitro activity is often not compatible with an improvement in cellular permeation parameters, in agreement with what has been reported by other authors developing small molecules directed at TAR recognition.

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

TABARRINI, Oriana;MASSARI, SERENA;SABATINI, STEFANO;FRAVOLINI, Arnaldo;CECCHETTI, Violetta
2009

Abstract

We have synthesized an extended series of 2-PQs, tested their activity on the Tat–TAR complex, and obtained novel compounds that exhibit higher activity while expanding our structure–activity analysis study for this new class of inhibitors. Our results demonstrate that the achievement of in vitro activity is often not compatible with an improvement in cellular permeation parameters, in agreement with what has been reported by other authors developing small molecules directed at TAR recognition.
File in questo prodotto:
Non ci sono file associati a questo prodotto.

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11391/152586
Citazioni
  • ???jsp.display-item.citation.pmc??? ND
  • Scopus 18
  • ???jsp.display-item.citation.isi??? 17
social impact