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Literature summary for 1.10.5.1 extracted from

  • Hussein, B.; Ikhmais, B.; Kadirvel, M.; Magwaza, R.N.; Halbert, G.; Bryce, R.A.; Stratford, I.J.; Freeman, S.
    Discovery of potent 4-aminoquinoline hydrazone inhibitors of NRH quinoneoxidoreductase-2 (NQO2) (2019), Eur. J. Med. Chem., 182, 111649 .
    View publication on PubMed
Search for more literature for 1.10.5.1

Inhibitors

Inhibitors Comment Organism Structure
2-methoxy-6-((2-(6-methoxy-2-methylquinolin-4-yl)hydrazono)methyl)phenol
-
 Homo sapiens
3-[(Z)-(6-methoxy-2-methylquinolin-4-yl)diazenyl]phenol
-
 Homo sapiens
4-[(Z)-(1H-imidazol-4-yl)diazenyl]-6-methoxy-2-methylquinoline
-
 Homo sapiens
4-[(Z)-(4-fluorophenyl)diazenyl]-6-methoxy-2-methylquinoline
-
 Homo sapiens
4-[(Z)-(6-methoxy-2-methylquinolin-4-yl)diazenyl]benzoic acid
-
 Homo sapiens
4-[(Z)-(6-methoxy-2-methylquinolin-4-yl)diazenyl]phenol
-
 Homo sapiens
4-[(Z)-benzyldiazenyl]-6-methoxy-2-methylquinoline
-
 Homo sapiens
4-[(Z)-[(1H-imidazol-4-yl)methyl]diazenyl]-6-methoxy-2-methylquinoline
-
 Homo sapiens
5-[(Z)-(6-methoxy-2-methylquinolin-4-yl)diazenyl]benzene-1,3-diol
-
 Homo sapiens
6-methoxy-2-methyl-4-[(Z)-(4-nitrophenyl)diazenyl]quinoline
-
 Homo sapiens
6-methoxy-2-methyl-4-[(Z)-(5-nitrofuran-2-yl)diazenyl]quinoline
-
 Homo sapiens
6-methoxy-2-methyl-4-[(Z)-(pyridin-3-yl)diazenyl]quinoline
-
 Homo sapiens
additional information study on 4-aminoquinoline hydrazone inhibitors. A small substituent at the 2-position of the 4-aminoquinoline ring is important to reduce steric hindrance and improve engagement of the scaffold within the NQO2 active site. Both the hydrazone and hydrazide derivatives are functionally active as inhibitors of NQO2 in the cells Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P16083
-
-

Source Tissue

Source Tissue Comment Organism Textmining
SKOV-3 cell high expression level of NQO2 Homo sapiens
-
TOV-112D cell low expression level of NQO2 Homo sapiens
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.01
-
 pH 7.4, 37°C Homo sapiens 6-methoxy-2-methyl-4-[(Z)-(pyridin-3-yl)diazenyl]quinoline
0.013
-
 pH 7.4, 37°C Homo sapiens 2-methoxy-6-((2-(6-methoxy-2-methylquinolin-4-yl)hydrazono)methyl)phenol
0.015
-
 pH 7.4, 37°C Homo sapiens 4-[(Z)-benzyldiazenyl]-6-methoxy-2-methylquinoline
0.018
-
 pH 7.4, 37°C Homo sapiens 6-methoxy-2-methyl-4-[(Z)-(5-nitrofuran-2-yl)diazenyl]quinoline
0.046
-
 pH 7.4, 37°C Homo sapiens 5-[(Z)-(6-methoxy-2-methylquinolin-4-yl)diazenyl]benzene-1,3-diol
0.055
-
 pH 7.4, 37°C Homo sapiens 4-[(Z)-(6-methoxy-2-methylquinolin-4-yl)diazenyl]phenol
0.064
-
 pH 7.4, 37°C Homo sapiens 4-[(Z)-(6-methoxy-2-methylquinolin-4-yl)diazenyl]benzoic acid
0.071
-
 pH 7.4, 37°C Homo sapiens 4-[(Z)-(1H-imidazol-4-yl)diazenyl]-6-methoxy-2-methylquinoline
0.083
-
 pH 7.4, 37°C Homo sapiens 6-methoxy-2-methyl-4-[(Z)-(4-nitrophenyl)diazenyl]quinoline
0.09
-
 pH 7.4, 37°C Homo sapiens 4-[(Z)-[(1H-imidazol-4-yl)methyl]diazenyl]-6-methoxy-2-methylquinoline
0.103
-
 pH 7.4, 37°C Homo sapiens 4-[(Z)-(4-fluorophenyl)diazenyl]-6-methoxy-2-methylquinoline
0.125
-
 pH 7.4, 37°C Homo sapiens 3-[(Z)-(6-methoxy-2-methylquinolin-4-yl)diazenyl]phenol
0.137
-
 pH 7.4, 37°C Homo sapiens 3-[(Z)-(6-methoxy-2-methylquinolin-4-yl)diazenyl]phenol