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Literature summary 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

EC Number Inhibitors Comment Organism Structure
2.4.2.4 (E)-N'-(2,3-dimethoxybenzylidene)isoquinoline-3-carbohydrazide
-
 Escherichia coli
2.4.2.4 (E)-N'-(2,4-dichlorobenzylidene)isoquinoline-3-carbohydrazide
-
 Escherichia coli
2.4.2.4 (E)-N'-(2-cyanobenzylidene)isoquinoline-3-carbohydrazide
-
 Escherichia coli
2.4.2.4 (E)-N'-(2-nitrobenzylidene)isoquinoline-3-carbohydrazide
-
 Escherichia coli
2.4.2.4 (E)-N'-(3,5-dichloro-2-hydroxybenzylidene)isoquinoline-3-carbohydrazide
-
 Escherichia coli
2.4.2.4 (E)-N'-(3-cyanobenzylidene)isoquinoline-3-carbohydrazide
-
 Escherichia coli
2.4.2.4 (E)-N'-(3-hydroxy-5-methoxybenzylidene)isoquinoline-3-carbohydrazide
-
 Escherichia coli
2.4.2.4 (E)-N'-(4-chlorobenzylidene)isoquinoline-3-carbohydrazide
-
 Escherichia coli
2.4.2.4 (E)-N'-(4-cyanobenzylidene)isoquinoline-3-carbohydrazide
-
 Escherichia coli
2.4.2.4 (E)-N'-(4-nitrobenzylidene)isoquinoline-3-carbohydrazide
-
 Escherichia coli
2.4.2.4 (E)-N'-(5-bromo-2-methoxybenzlidene)isoquinoline-3-carbohydrazide
-
 Escherichia coli
2.4.2.4 (E)-N'-(anthracen-9-ylmethylen)isoquinoline-3-carbohydrazide
-
 Escherichia coli
2.4.2.4 (Z)-N'-(1-(4-nitrophenyl)ethylidene)isoquinoline-3-carbohydrazide
-
 Escherichia coli
2.4.2.4 (Z)-N'-(3-chloro-4-hydroxybenzylidene)isoquinoline-3-carbohydrazide
-
 Escherichia coli
2.4.2.4 (Z)-N'-(4-hydroxy-3,5-dimethoxybenzylidene)isoquinoline-3-carbohydrazide
-
 Escherichia coli
2.4.2.4 5-chloro-6-[1-(2-iminopyrrolidinyl)methyl] uracil hydrochloride TPI Escherichia coli
2.4.2.4 7-deazaxanthine 7DX Escherichia coli
2.4.2.4 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)

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

Organism

EC Number Organism UniProt Comment Textmining
2.4.2.4 Escherichia coli P0C037
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.4.2.4 commercial preparation
-
 Escherichia coli
-

Substrates and Products (Substrate)

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

Synonyms

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

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.4.2.4 25
-
 assay at Escherichia coli

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.4.2.4 7.4
-
 assay at Escherichia coli

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.4.2.4 0.0044
-
 pH 7.4, 25°C Escherichia coli (Z)-N'-(4-hydroxy-3,5-dimethoxybenzylidene)isoquinoline-3-carbohydrazide
2.4.2.4 0.0081
-
 pH 7.4, 25°C Escherichia coli (E)-N'-(3,5-dichloro-2-hydroxybenzylidene)isoquinoline-3-carbohydrazide
2.4.2.4 0.0081
-
 pH 7.4, 25°C Escherichia coli (Z)-N'-(3-chloro-4-hydroxybenzylidene)isoquinoline-3-carbohydrazide
2.4.2.4 0.0086
-
 pH 7.4, 25°C Escherichia coli (E)-N'-(2,4-dichlorobenzylidene)isoquinoline-3-carbohydrazide
2.4.2.4 0.0113
-
 pH 7.4, 25°C Escherichia coli (E)-N'-(2-nitrobenzylidene)isoquinoline-3-carbohydrazide
2.4.2.4 0.0161
-
 pH 7.4, 25°C Escherichia coli (E)-N'-(3-hydroxy-5-methoxybenzylidene)isoquinoline-3-carbohydrazide
2.4.2.4 0.0184
-
 pH 7.4, 25°C Escherichia coli (E)-N'-(2-cyanobenzylidene)isoquinoline-3-carbohydrazide
2.4.2.4 0.0184
-
 pH 7.4, 25°C Escherichia coli (E)-N'-(4-chlorobenzylidene)isoquinoline-3-carbohydrazide
2.4.2.4 0.0214
-
 pH 7.4, 25°C Escherichia coli (E)-N'-(4-nitrobenzylidene)isoquinoline-3-carbohydrazide
2.4.2.4 0.0222
-
 pH 7.4, 25°C Escherichia coli (E)-N'-(4-cyanobenzylidene)isoquinoline-3-carbohydrazide
2.4.2.4 0.0276
-
 pH 7.4, 25°C Escherichia coli (Z)-N'-(1-(4-nitrophenyl)ethylidene)isoquinoline-3-carbohydrazide
2.4.2.4 0.0361
-
 pH 7.4, 25°C Escherichia coli (E)-N'-(3-cyanobenzylidene)isoquinoline-3-carbohydrazide
2.4.2.4 0.03868
-
 pH 7.4, 25°C Escherichia coli 7-deazaxanthine
2.4.2.4 0.0394
-
 pH 7.4, 25°C Escherichia coli (E)-N'-(2,3-dimethoxybenzylidene)isoquinoline-3-carbohydrazide
2.4.2.4 0.0447
-
 pH 7.4, 25°C Escherichia coli (E)-N'-(5-bromo-2-methoxybenzlidene)isoquinoline-3-carbohydrazide
2.4.2.4 0.0693
-
 pH 7.4, 25°C Escherichia coli (E)-N'-(anthracen-9-ylmethylen)isoquinoline-3-carbohydrazide

General Information

EC Number General Information Comment Organism
2.4.2.4 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