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Literature summary extracted from

  • Petrovic, M.; Roschger, C.; Chaudary, S.; Zierer, A.; Mladenovic, M.; Jakovljevic, K.; Markovic, V.; Botta, B.; Joksovic, M.
    Potent human dihydroorotate dehydrogenase inhibitory activity of new quinoline-4-carboxylic acids derived from phenolic aldehydes synthesis, cytotoxicity, lipophilicity and molecular docking studies (2020), Bioorg. Chem., 105, 104373 .
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.3.5.2 2-(2,3-bis(benzyloxy)phenyl)quinoline-4-carboxylic acid
-
 Homo sapiens
1.3.5.2 2-(2,4-bis(benzyloxy)phenyl)quinoline-4-carboxylic acid
-
 Homo sapiens
1.3.5.2 2-(2,4-dimethoxyphenyl)quinoline-4-carboxylic acid
-
 Homo sapiens
1.3.5.2 2-(3,4-bis(benzyloxy)phenyl)quinoline-4-carboxylic acid
-
 Homo sapiens
1.3.5.2 2-(3,4-dibutoxyphenyl)quinoline-4-carboxylic acid
-
 Homo sapiens
1.3.5.2 2-(3,4-dihydroxyphenyl)quinoline-4-carboxylic acid
-
 Homo sapiens
1.3.5.2 2-(3,4-diisobutoxyphenyl)quinoline-4-carboxylic acid
-
 Homo sapiens
1.3.5.2 2-(3,4-dimethoxyphenyl)quinoline-4-carboxylic acid
-
 Homo sapiens
1.3.5.2 2-(3,4-dipropoxyphenyl)quinoline-4-carboxylic acid
-
 Homo sapiens
1.3.5.2 2-(3-methoxy-4-propoxyphenyl)quinoline-4-carboxylic acid
-
 Homo sapiens
1.3.5.2 2-(4-(benzyloxy)-3-methoxyphenyl)quinoline-4-carboxylic acid
-
 Homo sapiens
1.3.5.2 2-(4-butoxy-3-methoxyphenyl)quinoline-4-carboxylic acid
-
 Homo sapiens
1.3.5.2 2-(4-hydroxy-3-methoxyphenyl)quinoline-4-carboxylic acid
-
 Homo sapiens
1.3.5.2 2-(4-isobutoxy-3-methoxyphenyl)quinoline-4-carboxylic acid
-
 Homo sapiens
1.3.5.2 6-fluoro-2-[2-methyl-4-phenoxy-5-(propan-2-yl)phenyl]quinoline-4-carboxylic acid i.e. C44 Homo sapiens
1.3.5.2 brequinar
-
 Homo sapiens
1.3.5.2 leflunomide
-
 Homo sapiens
1.3.5.2 additional information synthesis of a series of 2-substituted quinoline-4-carboxylic acids by Doebner reaction starting from freely available protocatechuic aldehyde and vanillin precursors. Human dihydroorotate dehydrogenase (hDHODH) is recognised as a clear molecular target for these heterocycles. All compounds are also tested for their antiproliferative potential against three cancer cells (MCF-7, A549, A375) and one normal cell line (HaCaT) to evaluate the selective cytotoxicity, overview. IC50 for cytotoxicity in in vivo assays. Molecular docking studies Homo sapiens
1.3.5.2 teriflunomide
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.3.5.2 (S)-dihydroorotate + decylubiquinone Homo sapiens
-
 orotate + decylubiquinol
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
1.3.5.2 Homo sapiens Q02127
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.3.5.2 (S)-dihydroorotate + decylubiquinone
-
 Homo sapiens orotate + decylubiquinol
-
 ?
1.3.5.2 additional information reduction of decylubiquinone (DUQ) is stoichiometrically equivalent to reduction of 2,6-ichloroindophenol (DCIP) resulting in the decrease in absorbance at 610 nm, which is measured Homo sapiens ?
-
-

Synonyms

EC Number Synonyms Comment Organism
1.3.5.2 dihydroorotate dehydrogenase
-
 Homo sapiens
1.3.5.2 hDHODH
-
 Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
1.3.5.2 22
-
 assay at room temperature Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
1.3.5.2 8
-
 assay at Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
1.3.5.2 decylubiquinone
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.3.5.2 0.00001
-
 pH 8.0, 22°C Homo sapiens brequinar
1.3.5.2 0.0009
-
 pH 8.0, 22°C Homo sapiens leflunomide
1.3.5.2 0.148
-
 pH 8.0, 22°C Homo sapiens 2-(3,4-diisobutoxyphenyl)quinoline-4-carboxylic acid
1.3.5.2 0.153
-
 pH 8.0, 22°C Homo sapiens 2-(3,4-dibutoxyphenyl)quinoline-4-carboxylic acid
1.3.5.2 0.268
-
 pH 8.0, 22°C Homo sapiens 2-(2,3-bis(benzyloxy)phenyl)quinoline-4-carboxylic acid
1.3.5.2 0.27
-
 pH 8.0, 22°C Homo sapiens 2-(3,4-bis(benzyloxy)phenyl)quinoline-4-carboxylic acid
1.3.5.2 0.34
-
 pH 8.0, 22°C Homo sapiens 2-(2,4-bis(benzyloxy)phenyl)quinoline-4-carboxylic acid
1.3.5.2 0.34
-
 pH 8.0, 22°C Homo sapiens 2-(4-butoxy-3-methoxyphenyl)quinoline-4-carboxylic acid
1.3.5.2 0.384
-
 pH 8.0, 22°C Homo sapiens 2-(3,4-dipropoxyphenyl)quinoline-4-carboxylic acid
1.3.5.2 0.438
-
 pH 8.0, 22°C Homo sapiens 2-(4-isobutoxy-3-methoxyphenyl)quinoline-4-carboxylic acid
1.3.5.2 0.449
-
 pH 8.0, 22°C Homo sapiens 2-(3-methoxy-4-propoxyphenyl)quinoline-4-carboxylic acid
1.3.5.2 0.467
-
 pH 8.0, 22°C Homo sapiens 2-(4-(benzyloxy)-3-methoxyphenyl)quinoline-4-carboxylic acid
1.3.5.2 0.944
-
 pH 8.0, 22°C Homo sapiens 2-(4-hydroxy-3-methoxyphenyl)quinoline-4-carboxylic acid
1.3.5.2 1.073
-
 pH 8.0, 22°C Homo sapiens 2-(3,4-dihydroxyphenyl)quinoline-4-carboxylic acid
1.3.5.2 1.387
-
 pH 8.0, 22°C Homo sapiens 2-(3,4-dimethoxyphenyl)quinoline-4-carboxylic acid
1.3.5.2 2.549
-
 pH 8.0, 22°C Homo sapiens 2-(2,4-dimethoxyphenyl)quinoline-4-carboxylic acid