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Literature summary for 3.1.13.2 extracted from

  • Billamboz, M.; Bailly, F.; Barreca, M.L.; De Luca, L.; Mouscadet, J.F.; Calmels, C.; Andreola, M.L.; Witvrouw, M.; Christ, F.; Debyser, Z.; Cotelle, P.
    Design, synthesis, and biological evaluation of a series of 2-hydroxyisoquinoline-1,3(2H,4H)-diones as dual inhibitors of human immunodeficiency virus type 1 integrase and the reverse transcriptase RNase H domain (2008), J. Med. Chem., 51, 7717-7730.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
2,7-dihydroxyisoquinoline-1,3(2H,4H)-dione
-
Human immunodeficiency virus 1
2-(4-fluorophenyl)-N-(2-hydroxy-1,3-dioxo-1,2,3,4-tetrahydroisoquinolin-7-yl)acetamide
-
Human immunodeficiency virus 1
2-hydroxy-7-(4-hydroxyphenyl)isoquinoline-1,3(2H,4H)-dione
-
Human immunodeficiency virus 1
2-hydroxy-7-iodoisoquinoline-1,3(2H,4H)-dione
-
Human immunodeficiency virus 1
2-hydroxy-7-nitroisoquinoline-1,3(2H,4H)-dione
-
Human immunodeficiency virus 1
2-hydroxy-7-phenylisoquinoline-1,3(2H,4H)-dione
-
Human immunodeficiency virus 1
2-hydroxy-7-[4-(trifluoromethyl)phenyl]isoquinoline-1,3(2H,4H)-dione
-
Human immunodeficiency virus 1
2-hydroxyisoquinoline-1,3(2H,4H)-dione
-
Human immunodeficiency virus 1
7-(3,4-dihydroxyphenyl)-2-hydroxyisoquinoline-1,3(2H,4H)-dione
-
Human immunodeficiency virus 1
7-(4-fluorophenyl)-2-hydroxyisoquinoline-1,3(2H,4H)-dione
-
Human immunodeficiency virus 1
7-bromo-2-hydroxyisoquinoline-1,3(2H,4H)-dione
-
Human immunodeficiency virus 1
7-chloro-2-hydroxyisoquinoline-1,3(2H,4H)-dione
-
Human immunodeficiency virus 1
N-(2-hydroxy-1,3-dioxo-1,2,3,4-tetrahydroisoquinolin-7-yl)-2-phenylacetamide
-
Human immunodeficiency virus 1
N-(2-hydroxy-1,3-dioxo-1,2,3,4-tetrahydroisoquinolin-7-yl)-3-nitrobenzamide
-
Human immunodeficiency virus 1
N-(2-hydroxy-1,3-dioxo-1,2,3,4-tetrahydroisoquinolin-7-yl)-4-fluorobenzamide
-
Human immunodeficiency virus 1
N-(2-hydroxy-1,3-dioxo-1,2,3,4-tetrahydroisoquinolin-7-yl)acetamide
-
Human immunodeficiency virus 1
N-(2-hydroxy-1,3-dioxo-1,2,3,4-tetrahydroisoquinolin-7-yl)benzamide
-
Human immunodeficiency virus 1
N-(2-hydroxy-1,3-dioxo-1,2,3,4-tetrahydroisoquinolin-7-yl)pentanamide
-
Human immunodeficiency virus 1

Organism

Organism UniProt Comment Textmining
Human immunodeficiency virus 1
-
-
-

Synonyms

Synonyms Comment Organism
HIV-1 RT ribonuclease H
-
Human immunodeficiency virus 1
RNase H reverse transcriptase RNase H domain Human immunodeficiency virus 1

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
additional information
-
IC50 value is higher than 96.00 microM for 7-bromo-2-hydroxyisoquinoline-1,3(2H,4H)-dione. IC50 value is higher than 80.0 microM for N-(2-hydroxy-1,3-dioxo-1,2,3,4-tetrahydroisoquinolin-7-yl)pentanamide, for 2-hydroxy-7-phenylisoquinoline-1,3(2H,4H)-dione, and for N-(2-hydroxy-1,3-dioxo-1,2,3,4-tetrahydroisoquinolin-7-yl)-2-phenylacetamide. pH 8.0, 37°C Human immunodeficiency virus 1 additional information
0.0057
-
pH 8.0, 37°C Human immunodeficiency virus 1 N-(2-hydroxy-1,3-dioxo-1,2,3,4-tetrahydroisoquinolin-7-yl)benzamide
0.0059
-
pH 8.0, 37°C Human immunodeficiency virus 1 2-hydroxyisoquinoline-1,3(2H,4H)-dione
0.0066
-
pH 8.0, 37°C Human immunodeficiency virus 1 7-(3,4-dihydroxyphenyl)-2-hydroxyisoquinoline-1,3(2H,4H)-dione
0.0071
-
pH 8.0, 37°C Human immunodeficiency virus 1 N-(2-hydroxy-1,3-dioxo-1,2,3,4-tetrahydroisoquinolin-7-yl)-4-fluorobenzamide
0.0072
-
pH 8.0, 37°C Human immunodeficiency virus 1 2-hydroxy-7-(4-hydroxyphenyl)isoquinoline-1,3(2H,4H)-dione
0.0107
-
pH 8.0, 37°C Human immunodeficiency virus 1 2-hydroxy-7-[4-(trifluoromethyl)phenyl]isoquinoline-1,3(2H,4H)-dione
0.0108
-
pH 8.0, 37°C Human immunodeficiency virus 1 N-(2-hydroxy-1,3-dioxo-1,2,3,4-tetrahydroisoquinolin-7-yl)-3-nitrobenzamide
0.0222
-
pH 8.0, 37°C Human immunodeficiency virus 1 7-(4-fluorophenyl)-2-hydroxyisoquinoline-1,3(2H,4H)-dione
0.0289
-
pH 8.0, 37°C Human immunodeficiency virus 1 7-chloro-2-hydroxyisoquinoline-1,3(2H,4H)-dione
0.0353
-
pH 8.0, 37°C Human immunodeficiency virus 1 2-(4-fluorophenyl)-N-(2-hydroxy-1,3-dioxo-1,2,3,4-tetrahydroisoquinolin-7-yl)acetamide
0.0374
-
pH 8.0, 37°C Human immunodeficiency virus 1 2,7-dihydroxyisoquinoline-1,3(2H,4H)-dione
0.0407
-
pH 8.0, 37°C Human immunodeficiency virus 1 N-(2-hydroxy-1,3-dioxo-1,2,3,4-tetrahydroisoquinolin-7-yl)acetamide
0.048
-
pH 8.0, 37°C Human immunodeficiency virus 1 2-hydroxy-7-nitroisoquinoline-1,3(2H,4H)-dione
0.058
-
pH 8.0, 37°C Human immunodeficiency virus 1 2-hydroxy-7-iodoisoquinoline-1,3(2H,4H)-dione