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Literature summary for 2.4.2.4 extracted from

  • Zhao, S.; Li, K.; Jin, Y.; Lin, J.
    Synthesis and biological evaluation of novel 1-(aryl-aldehyde-oxime)uracil derivatives as a new class of thymidine phosphorylase inhibitors (2018), Eur. J. Med. Chem., 144, 41-51 .
    View publication on PubMed
Search for more literature for 2.4.2.4

Inhibitors

Inhibitors Comment Organism Structure
(E)-1-((2-fluorophenyl)(hydroxyimino)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
(E)-1-((4-chlorophenyl)(hydroxyimino)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
(E)-1-((4-ethylphenyl)(hydroxyimino)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
(E)-1-((4-fluorophenyl)(hydroxyimino)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
(E)-1-((hydroxyimino)(3-methoxyphenyl)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
(E)-1-((hydroxyimino)(4-methoxyphenyl)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
(E)-1-((hydroxyimino)(p-tolyl)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
(E)-1-((hydroxyimino)(phenyl)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
(Z)-1-((2-fluorophenyl)(hydroxyimino)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
(Z)-1-((3,4-dichlorophenyl)(hydroxyimino)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
(Z)-1-((3-fluorophenyl)(hydroxyimino)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
(Z)-1-((4-bromophenyl)(hydroxyimino)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
(Z)-1-((4-chlorophenyl)(hydroxyimino)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
(Z)-1-((4-ethylphenyl)(hydroxyimino)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
(Z)-1-((4-fluorophenyl)(hydroxyimino)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
(Z)-1-((hydroxyimino)(3-methoxyphenyl)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
(Z)-1-((hydroxyimino)(4-methoxyphenyl)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
(Z)-1-((hydroxyimino)(m-tolyl)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
(Z)-1-((hydroxyimino)(p-tolyl)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
(Z)-1-((hydroxyimino)(phenyl)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
(Z)-1-((hydroxyimino)(thiophen-2-yl)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
1-((methoxyimino)(phenyl)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
1-benzoyl-6-methylpyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
7-deazaxanthine
-
 Homo sapiens
additional information synthesis and biological evaluation of 1-(aryl-aldehyde-oxime)uracil derivatives as a class of thymidine phosphorylase inhibitors, molecular docking and binding energies, overview. The crystal structure of thymidine phosphorylase (PDB ID 1UOU) is used as protein receptor in molecular docking Homo sapiens
TPI
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens P19971
-
-

Source Tissue

Source Tissue Comment Organism Textmining
umbilical vein endothelial cell HUVEC Homo sapiens
-

Substrates and Products (Substrate)

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

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
30 37 assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
8.4
-
 assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00003
-
 pH 8.4, 30°C Homo sapiens TPI
0.00012
-
 pH 8.4, 30°C Homo sapiens (Z)-1-((3,4-dichlorophenyl)(hydroxyimino)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
0.0014
-
 pH 8.4, 30°C Homo sapiens (Z)-1-((4-chlorophenyl)(hydroxyimino)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
0.0027
-
 pH 8.4, 30°C Homo sapiens (Z)-1-((4-bromophenyl)(hydroxyimino)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
0.0034
-
 pH 8.4, 30°C Homo sapiens (Z)-1-((4-ethylphenyl)(hydroxyimino)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
0.0072
-
 pH 8.4, 30°C Homo sapiens (Z)-1-((hydroxyimino)(p-tolyl)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
0.0107
-
 pH 8.4, 30°C Homo sapiens (E)-1-((4-ethylphenyl)(hydroxyimino)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
0.0156
-
 pH 8.4, 30°C Homo sapiens (E)-1-((4-chlorophenyl)(hydroxyimino)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
0.0159
-
 pH 8.4, 30°C Homo sapiens (Z)-1-((hydroxyimino)(m-tolyl)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
0.0165
-
 pH 8.4, 30°C Homo sapiens (Z)-1-((hydroxyimino)(4-methoxyphenyl)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
0.0214
-
 pH 8.4, 30°C Homo sapiens (Z)-1-((hydroxyimino)(phenyl)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
0.0225
-
 pH 8.4, 30°C Homo sapiens (E)-1-((hydroxyimino)(p-tolyl)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
0.0251
-
 pH 8.4, 30°C Homo sapiens (Z)-1-((hydroxyimino)(3-methoxyphenyl)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
0.0252
-
 pH 8.4, 30°C Homo sapiens (E)-1-((hydroxyimino)(4-methoxyphenyl)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
0.0334
-
 pH 8.4, 30°C Homo sapiens (E)-1-((hydroxyimino)(3-methoxyphenyl)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
0.0373
-
 pH 8.4, 30°C Homo sapiens (E)-1-((hydroxyimino)(phenyl)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
0.0399
-
 pH 8.4, 30°C Homo sapiens (Z)-1-((hydroxyimino)(thiophen-2-yl)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
0.0403
-
 pH 8.4, 30°C Homo sapiens 7-deazaxanthine
0.0412
-
 pH 8.4, 30°C Homo sapiens (Z)-1-((3-fluorophenyl)(hydroxyimino)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
0.0413
-
 pH 8.4, 30°C Homo sapiens (E)-1-((4-fluorophenyl)(hydroxyimino)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
0.0441
-
 pH 8.4, 30°C Homo sapiens (Z)-1-((4-fluorophenyl)(hydroxyimino)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
0.0493
-
 pH 8.4, 30°C Homo sapiens (Z)-1-((2-fluorophenyl)(hydroxyimino)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
0.0537
-
 pH 8.4, 30°C Homo sapiens (E)-1-((2-fluorophenyl)(hydroxyimino)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
0.0856
-
 pH 8.4, 30°C Homo sapiens 1-((methoxyimino)(phenyl)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
0.0924
-
 pH 8.4, 30°C Homo sapiens 1-benzoyl-6-methylpyrimidine-2,4(1H,3H)-dione