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Literature summary for 2.4.2.4 extracted from

  • Zaman, K.; Rahim, F.; Taha, M.; Wadood, A.; Adnan Ali Shah, S.; Gollapalli, M.; Ullah, F.; Ahmed, A.
    Synthesis, thymidine phosphorylase, angiogenic inhibition and molecular docking study of isoquinoline derivatives (2019), Bioorg. Chem., 89, 102999 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(E)-N'-(2,3-dimethoxybenzylidene)isoquinoline-3-carbohydrazide
-
Escherichia coli
(E)-N'-(2,4-dichlorobenzylidene)isoquinoline-3-carbohydrazide
-
Escherichia coli
(E)-N'-(2-cyanobenzylidene)isoquinoline-3-carbohydrazide
-
Escherichia coli
(E)-N'-(2-nitrobenzylidene)isoquinoline-3-carbohydrazide
-
Escherichia coli
(E)-N'-(3,5-dichloro-2-hydroxybenzylidene)isoquinoline-3-carbohydrazide
-
Escherichia coli
(E)-N'-(3-cyanobenzylidene)isoquinoline-3-carbohydrazide
-
Escherichia coli
(E)-N'-(3-hydroxy-5-methoxybenzylidene)isoquinoline-3-carbohydrazide
-
Escherichia coli
(E)-N'-(4-chlorobenzylidene)isoquinoline-3-carbohydrazide
-
Escherichia coli
(E)-N'-(4-cyanobenzylidene)isoquinoline-3-carbohydrazide
-
Escherichia coli
(E)-N'-(4-nitrobenzylidene)isoquinoline-3-carbohydrazide
-
Escherichia coli
(E)-N'-(5-bromo-2-methoxybenzlidene)isoquinoline-3-carbohydrazide
-
Escherichia coli
(E)-N'-(anthracen-9-ylmethylen)isoquinoline-3-carbohydrazide
-
Escherichia coli
(Z)-N'-(1-(4-nitrophenyl)ethylidene)isoquinoline-3-carbohydrazide
-
Escherichia coli
(Z)-N'-(3-chloro-4-hydroxybenzylidene)isoquinoline-3-carbohydrazide
-
Escherichia coli
(Z)-N'-(4-hydroxy-3,5-dimethoxybenzylidene)isoquinoline-3-carbohydrazide
-
Escherichia coli
5-chloro-6-[1-(2-iminopyrrolidinyl)methyl] uracil hydrochloride TPI Escherichia coli
7-deazaxanthine 7DX Escherichia coli
additional information in vitro study of thymidine phosphorylase inhibition, overview. Sixteen analogs of N-benzyliden-isoquinoline-3-carbohydrazide are synthesized and evaluated their inhibitory activity against thymidine phosphorylase enzyme, molecular docking study using structure with PDB ID 4EAD as template. No inhibition by (Z)-N'-(3-methoxy-4-(phenoxymethyl)benzylidene)isoquinoline-3-carbohydrazide Escherichia coli

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 Escherichia coli
-
thymidine + phosphate
-
r
uracil + 2-deoxy-alpha-D-ribose 1-phosphate Escherichia coli
-
2'-deoxyuridine + phosphate
-
r

Organism

Organism UniProt Comment Textmining
Escherichia coli P0C037
-
-

Source Tissue

Source Tissue Comment Organism Textmining
commercial preparation
-
Escherichia coli
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
Escherichia coli thymidine + phosphate
-
r
uracil + 2-deoxy-alpha-D-ribose 1-phosphate
-
Escherichia coli 2'-deoxyuridine + phosphate
-
r

Synonyms

Synonyms Comment Organism
ppnP
-
Escherichia coli
pyrimidine/purine nucleoside phosphorylase
-
Escherichia coli

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
25
-
assay at Escherichia coli

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
assay at Escherichia coli

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0044
-
pH 7.4, 25°C Escherichia coli (Z)-N'-(4-hydroxy-3,5-dimethoxybenzylidene)isoquinoline-3-carbohydrazide
0.0081
-
pH 7.4, 25°C Escherichia coli (E)-N'-(3,5-dichloro-2-hydroxybenzylidene)isoquinoline-3-carbohydrazide
0.0081
-
pH 7.4, 25°C Escherichia coli (Z)-N'-(3-chloro-4-hydroxybenzylidene)isoquinoline-3-carbohydrazide
0.0086
-
pH 7.4, 25°C Escherichia coli (E)-N'-(2,4-dichlorobenzylidene)isoquinoline-3-carbohydrazide
0.0113
-
pH 7.4, 25°C Escherichia coli (E)-N'-(2-nitrobenzylidene)isoquinoline-3-carbohydrazide
0.0161
-
pH 7.4, 25°C Escherichia coli (E)-N'-(3-hydroxy-5-methoxybenzylidene)isoquinoline-3-carbohydrazide
0.0184
-
pH 7.4, 25°C Escherichia coli (E)-N'-(2-cyanobenzylidene)isoquinoline-3-carbohydrazide
0.0184
-
pH 7.4, 25°C Escherichia coli (E)-N'-(4-chlorobenzylidene)isoquinoline-3-carbohydrazide
0.0214
-
pH 7.4, 25°C Escherichia coli (E)-N'-(4-nitrobenzylidene)isoquinoline-3-carbohydrazide
0.0222
-
pH 7.4, 25°C Escherichia coli (E)-N'-(4-cyanobenzylidene)isoquinoline-3-carbohydrazide
0.0276
-
pH 7.4, 25°C Escherichia coli (Z)-N'-(1-(4-nitrophenyl)ethylidene)isoquinoline-3-carbohydrazide
0.0361
-
pH 7.4, 25°C Escherichia coli (E)-N'-(3-cyanobenzylidene)isoquinoline-3-carbohydrazide
0.03868
-
pH 7.4, 25°C Escherichia coli 7-deazaxanthine
0.0394
-
pH 7.4, 25°C Escherichia coli (E)-N'-(2,3-dimethoxybenzylidene)isoquinoline-3-carbohydrazide
0.0447
-
pH 7.4, 25°C Escherichia coli (E)-N'-(5-bromo-2-methoxybenzlidene)isoquinoline-3-carbohydrazide
0.0693
-
pH 7.4, 25°C Escherichia coli (E)-N'-(anthracen-9-ylmethylen)isoquinoline-3-carbohydrazide

General Information

General Information Comment Organism
metabolism thymidine phosphorylase (TP) is the key enzyme of the pyrimidine salvage pathway, which speedup the conversion of thymidine and 2'-deoxyuridine to their respective bases and 2-deoxy-D-ribose 1-phosphate Escherichia coli