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Literature summary 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

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.4.2.4 (E)-1-((2-fluorophenyl)(hydroxyimino)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
2.4.2.4 (E)-1-((4-chlorophenyl)(hydroxyimino)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
2.4.2.4 (E)-1-((4-ethylphenyl)(hydroxyimino)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
2.4.2.4 (E)-1-((4-fluorophenyl)(hydroxyimino)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
2.4.2.4 (E)-1-((hydroxyimino)(3-methoxyphenyl)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
2.4.2.4 (E)-1-((hydroxyimino)(4-methoxyphenyl)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
2.4.2.4 (E)-1-((hydroxyimino)(p-tolyl)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
2.4.2.4 (E)-1-((hydroxyimino)(phenyl)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
2.4.2.4 (Z)-1-((2-fluorophenyl)(hydroxyimino)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
2.4.2.4 (Z)-1-((3,4-dichlorophenyl)(hydroxyimino)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
2.4.2.4 (Z)-1-((3-fluorophenyl)(hydroxyimino)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
2.4.2.4 (Z)-1-((4-bromophenyl)(hydroxyimino)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
2.4.2.4 (Z)-1-((4-chlorophenyl)(hydroxyimino)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
2.4.2.4 (Z)-1-((4-ethylphenyl)(hydroxyimino)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
2.4.2.4 (Z)-1-((4-fluorophenyl)(hydroxyimino)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
2.4.2.4 (Z)-1-((hydroxyimino)(3-methoxyphenyl)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
2.4.2.4 (Z)-1-((hydroxyimino)(4-methoxyphenyl)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
2.4.2.4 (Z)-1-((hydroxyimino)(m-tolyl)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
2.4.2.4 (Z)-1-((hydroxyimino)(p-tolyl)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
2.4.2.4 (Z)-1-((hydroxyimino)(phenyl)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
2.4.2.4 (Z)-1-((hydroxyimino)(thiophen-2-yl)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
2.4.2.4 1-((methoxyimino)(phenyl)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
2.4.2.4 1-benzoyl-6-methylpyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
2.4.2.4 7-deazaxanthine
-
 Homo sapiens
2.4.2.4 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
2.4.2.4 TPI
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

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

Organism

EC Number Organism UniProt Comment Textmining
2.4.2.4 Homo sapiens P19971
-
-

Source Tissue

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

Substrates and Products (Substrate)

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

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.4.2.4 30 37 assay at Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.4.2.4 8.4
-
 assay at Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.4.2.4 0.00003
-
 pH 8.4, 30°C Homo sapiens TPI
2.4.2.4 0.00012
-
 pH 8.4, 30°C Homo sapiens (Z)-1-((3,4-dichlorophenyl)(hydroxyimino)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
2.4.2.4 0.0014
-
 pH 8.4, 30°C Homo sapiens (Z)-1-((4-chlorophenyl)(hydroxyimino)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
2.4.2.4 0.0027
-
 pH 8.4, 30°C Homo sapiens (Z)-1-((4-bromophenyl)(hydroxyimino)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
2.4.2.4 0.0034
-
 pH 8.4, 30°C Homo sapiens (Z)-1-((4-ethylphenyl)(hydroxyimino)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
2.4.2.4 0.0072
-
 pH 8.4, 30°C Homo sapiens (Z)-1-((hydroxyimino)(p-tolyl)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
2.4.2.4 0.0107
-
 pH 8.4, 30°C Homo sapiens (E)-1-((4-ethylphenyl)(hydroxyimino)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
2.4.2.4 0.0156
-
 pH 8.4, 30°C Homo sapiens (E)-1-((4-chlorophenyl)(hydroxyimino)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
2.4.2.4 0.0159
-
 pH 8.4, 30°C Homo sapiens (Z)-1-((hydroxyimino)(m-tolyl)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
2.4.2.4 0.0165
-
 pH 8.4, 30°C Homo sapiens (Z)-1-((hydroxyimino)(4-methoxyphenyl)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
2.4.2.4 0.0214
-
 pH 8.4, 30°C Homo sapiens (Z)-1-((hydroxyimino)(phenyl)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
2.4.2.4 0.0225
-
 pH 8.4, 30°C Homo sapiens (E)-1-((hydroxyimino)(p-tolyl)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
2.4.2.4 0.0251
-
 pH 8.4, 30°C Homo sapiens (Z)-1-((hydroxyimino)(3-methoxyphenyl)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
2.4.2.4 0.0252
-
 pH 8.4, 30°C Homo sapiens (E)-1-((hydroxyimino)(4-methoxyphenyl)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
2.4.2.4 0.0334
-
 pH 8.4, 30°C Homo sapiens (E)-1-((hydroxyimino)(3-methoxyphenyl)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
2.4.2.4 0.0373
-
 pH 8.4, 30°C Homo sapiens (E)-1-((hydroxyimino)(phenyl)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
2.4.2.4 0.0399
-
 pH 8.4, 30°C Homo sapiens (Z)-1-((hydroxyimino)(thiophen-2-yl)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
2.4.2.4 0.0403
-
 pH 8.4, 30°C Homo sapiens 7-deazaxanthine
2.4.2.4 0.0412
-
 pH 8.4, 30°C Homo sapiens (Z)-1-((3-fluorophenyl)(hydroxyimino)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
2.4.2.4 0.0413
-
 pH 8.4, 30°C Homo sapiens (E)-1-((4-fluorophenyl)(hydroxyimino)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
2.4.2.4 0.0441
-
 pH 8.4, 30°C Homo sapiens (Z)-1-((4-fluorophenyl)(hydroxyimino)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
2.4.2.4 0.0493
-
 pH 8.4, 30°C Homo sapiens (Z)-1-((2-fluorophenyl)(hydroxyimino)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
2.4.2.4 0.0537
-
 pH 8.4, 30°C Homo sapiens (E)-1-((2-fluorophenyl)(hydroxyimino)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
2.4.2.4 0.0856
-
 pH 8.4, 30°C Homo sapiens 1-((methoxyimino)(phenyl)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
2.4.2.4 0.0924
-
 pH 8.4, 30°C Homo sapiens 1-benzoyl-6-methylpyrimidine-2,4(1H,3H)-dione