1598381-75-9Relevant academic research and scientific papers
Basic quinolinonyl diketo acid derivatives as inhibitors of HIV integrase and their activity against RNase H function of reverse transcriptase
Costi, Roberta,Métifiot, Mathieu,Chung, Suhman,Cuzzucoli Crucitti, Giuliana,Maddali, Kasthuraiah,Pescatori, Luca,Messore, Antonella,Madia, Valentina Noemi,Pupo, Giovanni,Scipione, Luigi,Tortorella, Silvano,Di Leva, Francesco Saverio,Cosconati, Sandro,Marinelli, Luciana,Novellino, Ettore,Le Grice, Stuart F. J.,Corona, Angela,Pommier, Yves,Marchand, Christophe,Di Santo, Roberto
, p. 3223 - 3234 (2014/05/20)
A series of antiviral basic quinolinonyl diketo acid derivatives were developed as inhibitors of HIV-1 IN. Compounds 12d,f,i inhibited HIV-1 IN with IC50 values below 100 nM for strand transfer and showed a 2 order of magnitude selectivity over 3′-processing. These strand transfer selective inhibitors also inhibited HIV-1 RNase H with low micromolar potencies. Molecular modeling studies based on both the HIV-1 IN and RNase H catalytic core domains provided new structural insights for the future development of these compounds as dual HIV-1 IN and RNase H inhibitors.
