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:
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