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Literature summary for 2.4.2.4 extracted from

  • Zaman, K.; Rahim, F.; Taha, M.; Wadood, A.; Shah, S.A.A.; Ahmed, Q.U.; Zakaria, Z.A.
    Synthesis of new isoquinoline-base-oxadiazole derivatives as potent inhibitors of thymidine phosphorylase and molecular docking study (2019), Sci. Rep., 9, 16015 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.4.2.4

Inhibitors

Inhibitors Comment Organism Structure
(Z)-N'-((4-chloro-2-oxo-4a,8a-dihydro-2H-chromen-3-yl)methylene)-2-oxo-1,2,4a,8a-tetrahydroquinoline-6-carbohydrazide
-
 Homo sapiens
3-(3-(quinoxalin-2-yl)thiazolo[2,3-c][1,2,4]triazol-5-yl)benzene-1,2-diol
-
 Homo sapiens
4-(2,5-difluorobenzyl)-N-(4-(trifluoromethyl)phenyl)piperazine-1-carbothioamide
-
 Homo sapiens
4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)-N'-(1-(4-nitrophenyl)ethylidene)benzohydrazide
-
 Homo sapiens
4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)-N'-(2,3,4-trihydroxybenzylidene)benzohydrazide
-
 Homo sapiens
4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)-N'-(2,3,4-trimethoxybenzylidene)benzohydrazide
-
 Homo sapiens
4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)-N'-(2-nitrobenzylidene)benzohydrazide
-
 Homo sapiens
4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)-N'-(3,4,5-trimethoxybenzylidene)benzohydrazide
-
 Homo sapiens
4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)-N'-(4-(phenoxymethyl)benzylidene)benzohydrazide
-
 Homo sapiens
7-deazaxanthine
-
 Homo sapiens
additional information synthesis of isoquinoline-base-oxadiazole derivatives as potent inhibitors of thymidine phosphorylase and molecular docking study, overview. Twenty derivatives of isoquinoline bearing oxadiazole are characterized through different spectroscopic techniques such as HREI-MS, 1H-NMR and 13C-NMR and evaluated for thymidine phosphorylase inhibition, structure-activity relationships study Homo sapiens
N'-(2,4-dichlorobenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
-
 Homo sapiens
N'-(2-cyanobenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
-
 Homo sapiens
N'-(2-hydroxy-3-methoxybenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
-
 Homo sapiens
N'-(3,5-dichloro-2-hydroxybenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
-
 Homo sapiens
N'-(3-aminobenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
-
 Homo sapiens
N'-(3-cyanobenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
-
 Homo sapiens
N'-(3-hydroxy-4-methoxybenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
-
 Homo sapiens
N'-(4-(dimethylamino)benzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
-
 Homo sapiens
N'-(4-chlorobenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
-
 Homo sapiens
N'-(4-cyanobenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
-
 Homo sapiens
N'-(4-hydroxy-3,5-dimethoxybenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
-
 Homo sapiens
N'-(4-hydroxy-3-methoxybenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
-
 Homo sapiens
N'-(5-bromo-2-methoxybenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
-
 Homo sapiens
N'-(anthracen-9-ylmethylene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
thymine + 2-deoxy-alpha-D-ribose 1-phosphate Homo sapiens
-
 thymidine + phosphate
-
 r

Organism

Organism UniProt Comment Textmining
Homo sapiens P19971
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
 Homo sapiens thymidine + phosphate
-
 r

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
25
-
 assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
 assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0011
-
 pH 7.4, 25°C Homo sapiens 4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)-N'-(2,3,4-trihydroxybenzylidene)benzohydrazide
0.0011
-
 pH 7.4, 25°C Homo sapiens N'-(3-aminobenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
0.0024
-
 pH 7.4, 25°C Homo sapiens N'-(3,5-dichloro-2-hydroxybenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
0.0033
-
 pH 7.4, 25°C Homo sapiens N'-(2,4-dichlorobenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
0.0046
-
 pH 7.4, 25°C Homo sapiens N'-(3-hydroxy-4-methoxybenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
0.0053
-
 pH 7.4, 25°C Homo sapiens N'-(4-hydroxy-3,5-dimethoxybenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
0.006
-
 pH 7.4, 25°C Homo sapiens N'-(4-hydroxy-3-methoxybenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
0.0063
-
 pH 7.4, 25°C Homo sapiens 4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)-N'-(2-nitrobenzylidene)benzohydrazide
0.0073
-
 pH 7.4, 25°C Homo sapiens N'-(2-hydroxy-3-methoxybenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
0.0146
-
 pH 7.4, 25°C Homo sapiens 4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)-N'-(1-(4-nitrophenyl)ethylidene)benzohydrazide
0.0164
-
 pH 7.4, 25°C Homo sapiens N'-(4-chlorobenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
0.0185
-
 pH 7.4, 25°C Homo sapiens N'-(2-cyanobenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
0.0188
-
 pH 7.4, 25°C Homo sapiens N'-(4-(dimethylamino)benzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
0.0221
-
 pH 7.4, 25°C Homo sapiens N'-(4-cyanobenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
0.0274
-
 pH 7.4, 25°C Homo sapiens N'-(3-cyanobenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
0.0283
-
 pH 7.4, 25°C Homo sapiens 4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)-N'-(4-(phenoxymethyl)benzylidene)benzohydrazide
0.0367
-
 pH 7.4, 25°C Homo sapiens N'-(5-bromo-2-methoxybenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
0.03868
-
 pH 7.4, 25°C Homo sapiens 7-deazaxanthine
0.0394
-
 pH 7.4, 25°C Homo sapiens N'-(anthracen-9-ylmethylene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
0.0473
-
 pH 7.4, 25°C Homo sapiens 4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)-N'-(3,4,5-trimethoxybenzylidene)benzohydrazide
0.0546
-
 pH 7.4, 25°C Homo sapiens 4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)-N'-(2,3,4-trimethoxybenzylidene)benzohydrazide

General Information

General Information Comment Organism
malfunction overexpression of thymidine phosphorylase (TP) causes diseases like psoriasis, chronic inflammatory disease, tumor angiogenesis and rheumatoid arthritis etc. The inhibition of this enzyme is vital to secure life from serious threats Homo sapiens