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Literature summary for 3.1.26.13 extracted from

  • Costi, R.; Metifiot, M.; Chung, S.; Cuzzucoli Crucitti, G.; Maddali, K.; Pescatori, L.; Messore, A.; Madia, V.N.; Pupo, G.; Scipione, L.; Tortorella, S.; Di Leva, F.S.; Cosconati, S.; Marinelli, L.; Novellino, E.; Le Grice, S.F.; Corona, A.; Pommier, Y.; Marchand, C.; Di Santo, R.
    Basic quinolinonyl diketo acid derivatives as inhibitors of HIV integrase and their activity against RNase H function of reverse transcriptase (2014), J. Med. Chem., 57, 3223-3234.
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
(2Z)-4-[1-(4-fluorobenzyl)-4-oxo-7-(pyrrolidin-1-yl)-1,4-dihydroquinolin-3-yl]-2-hydroxy-4-oxobut-2-enoic acid
-
Human immunodeficiency virus 1
10,12,15,16-tetrahydroxy-8-methoxy-11-methyl-2-phenyl-6,7-dihydrotetraceno[1,2-g]phthalazine-1,9,14(2H)-trione
-
Human immunodeficiency virus 1
2,3,7-trihydroxy-6-(3-nitrobenzyl)cyclohepta-2,4,6-trien-1-one
-
Human immunodeficiency virus 1
4-[1-4-[(4-fluorophenyl)methyl]-7-[N-(3-chloroprop-1-yl)-piperazin-1-yl]-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid ethyl ester 35% inhibition at 0.01 mM Human immunodeficiency virus 1
4-[1-[(4-fluorophenyl)methyl]-7-(dimethylamino)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid 72% inhibition at 0.01 mM Human immunodeficiency virus 1
4-[1-[(4-fluorophenyl)methyl]-7-(dimethylamino)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid ethyl ester 26% inhibition at 0.01 mM Human immunodeficiency virus 1
4-[1-[(4-fluorophenyl)methyl]-7-(morpholin-4-yl)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid ethyl ester 0.7% inhibition at 0.01 mM Human immunodeficiency virus 1
4-[1-[(4-fluorophenyl)methyl]-7-(N-acetylpiperazin-1-yl)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid 22% inhibition at 0.01 mM Human immunodeficiency virus 1
4-[1-[(4-fluorophenyl)methyl]-7-(N-acetylpiperazin-1-yl)-4-(1h)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid ethyl ester 30% inhibition at 0.01 mM Human immunodeficiency virus 1
4-[1-[(4-fluorophenyl)methyl]-7-(N-ethylpiperazin-1-yl)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid 34% inhibition at 0.01 mM Human immunodeficiency virus 1
4-[1-[(4-fluorophenyl)methyl]-7-(N-ethylpiperazin-1-yl)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid ethyl ester 63% inhibition at 0.01 mM Human immunodeficiency virus 1
4-[1-[(4-fluorophenyl)methyl]-7-(N-methylpiperazin-1-yl)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid 44% inhibition at 0.01 mM Human immunodeficiency virus 1
4-[1-[(4-fluorophenyl)methyl]-7-(N-methylpiperazin-1-yl)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid ethyl ester 41% inhibition at 0.01 mM Human immunodeficiency virus 1
4-[1-[(4-fluorophenyl)methyl]-7-(piperazin-1-yl)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid 44% inhibition at 0.01 mM Human immunodeficiency virus 1
4-[1-[(4-fluorophenyl)methyl]-7-(piperazin-1-yl)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid ethyl ester 18% inhibition at 0.01 mM Human immunodeficiency virus 1
4-[1-[(4-fluorophenyl)methyl]-7-(thiomorpholin-1-yl)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid 74% inhibition at 0.01 mM Human immunodeficiency virus 1
4-[1-[(4-fluorophenyl)methyl]-7-[N-(3-chloroprop-1-yl)piperazin-1-yl]-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid 78% inhibition at 0.01 mM Human immunodeficiency virus 1
ethyl (2Z)-4-[1-(4-fluorobenzyl)-4-oxo-7-(pyrrolidin-1-yl)-1,4-dihydroquinolin-3-yl]-2-hydroxy-4-oxobut-2-enoate
-
Human immunodeficiency virus 1
methyl 2-hydroxy-1,3-dioxo-1,2,3,4-tetrahydroisoquinoline-4-carboxylate
-
Human immunodeficiency virus 1

Organism

Organism UniProt Comment Textmining
Human immunodeficiency virus 1
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
RNA-DNA hybrid + H2O
-
Human immunodeficiency virus 1 ?
-
?

Synonyms

Synonyms Comment Organism
ribonuclease H
-
Human immunodeficiency virus 1
RNase H
-
Human immunodeficiency virus 1

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0033
-
in 50 mM Tris-HCl, pH 8.0, at 37°C Human immunodeficiency virus 1 4-[1-[(4-fluorophenyl)methyl]-7-(N-acetylpiperazin-1-yl)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid
0.0057
-
in 50 mM Tris-HCl, pH 8.0, at 37°C Human immunodeficiency virus 1 4-[1-[(4-fluorophenyl)methyl]-7-[N-(3-chloroprop-1-yl)piperazin-1-yl]-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid
0.0066
-
in 50 mM Tris-HCl, pH 8.0, at 37°C Human immunodeficiency virus 1 4-[1-[(4-fluorophenyl)methyl]-7-(dimethylamino)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid
0.0068
-
in 50 mM Tris-HCl, pH 8.0, at 37°C Human immunodeficiency virus 1 4-[1-[(4-fluorophenyl)methyl]-7-(morpholin-4-yl)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid ethyl ester
0.0185
-
in 50 mM Tris-HCl, pH 8.0, at 37°C Human immunodeficiency virus 1 4-[1-[(4-fluorophenyl)methyl]-7-(N-methylpiperazin-1-yl)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid ethyl ester
0.0262
-
in 50 mM Tris-HCl, pH 8.0, at 37°C Human immunodeficiency virus 1 4-[1-[(4-fluorophenyl)methyl]-7-(N-ethylpiperazin-1-yl)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid ethyl ester
0.0287
-
in 50 mM Tris-HCl, pH 8.0, at 37°C Human immunodeficiency virus 1 4-[1-[(4-fluorophenyl)methyl]-7-(piperazin-1-yl)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid