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Literature summary for 5.6.2.1 extracted from

  • Karki, R.; Thapa, P.; Kang, M.J.; Jeong, T.C.; Nam, J.M.; Kim, H.L.; Na, Y.; Cho, W.J.; Kwon, Y.; Lee, E.S.
    Synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship study of hydroxylated 2,4-diphenyl-6-aryl pyridines (2010), Bioorg. Med. Chem., 18, 3066-3077.
    View publication on PubMed
Search for more literature for 5.6.2.1

Inhibitors

Inhibitors Comment Organism Structure
3,3'-(4-phenylpyridine-2,6-diyl)diphenol 67.2% inhibition at 0.1 mM Homo sapiens
3-(2,6-diphenylpyridin-4-yl)phenol 11.5% inhibition at 0.1 mM Homo sapiens
3-(4,6-diphenylpyridin-2-yl)phenol 12.9% inhibition at 0.1 mM Homo sapiens
3-(4-phenyl-2,4'-bipyridin-6-yl)phenol 70.4% inhibition at 0.1 mM Homo sapiens
3-(6-phenyl-2,2'-bipyridin-4-yl)phenol 10.8% inhibition at 0.1 mM Homo sapiens
3-(6-phenyl-2,3'-bipyridin-4-yl)phenol 8.8% inhibition at 0.1 mM Homo sapiens
3-(6-phenyl-2,4'-bipyridin-4-yl)phenol 60.8% inhibition at 0.1 mM Homo sapiens
3-[2-(furan-2-yl)-6-phenylpyridin-4-yl]phenol 48.8% inhibition at 0.1 mM Homo sapiens
3-[2-phenyl-6-(thiophen-2-yl)pyridin-4-yl]phenol 9.1% inhibition at 0.1 mM Homo sapiens
3-[2-phenyl-6-(thiophen-3-yl)pyridin-4-yl]phenol 6.9% inhibition at 0.1 mM Homo sapiens
3-[4-phenyl-6-(thiophen-2-yl)pyridin-2-yl]phenol 51.2% inhibition at 0.1 mM Homo sapiens
3-[4-phenyl-6-(thiophen-3-yl)pyridin-2-yl]phenol 75.8% inhibition at 0.1 mM Homo sapiens
3-[6-(furan-2-yl)-4-phenylpyridin-2-yl]phenol 10.2% inhibition at 0.1 mM Homo sapiens
4-(4,6-diphenylpyridin-2-yl)phenol 52.9% inhibition at 0.1 mM Homo sapiens
4-(4-phenyl-2,3'-bipyridin-6-yl)phenol 44% inhibition at 0.1 mM Homo sapiens
4-(6-phenyl-2,4'-bipyridin-4-yl)phenol 57.5% inhibition at 0.1 mM Homo sapiens
4-[2-(furan-2-yl)-6-phenylpyridin-4-yl]phenol 5.0% inhibition at 0.1 mM Homo sapiens
4-[4-phenyl-6-(thiophen-2-yl)pyridin-2-yl]phenol 4.9% inhibition at 0.1 mM Homo sapiens
4-[4-phenyl-6-(thiophen-3-yl)pyridin-2-yl]phenol 20.4% inhibition at 0.1 mM Homo sapiens
4-[6-(furan-2-yl)-4-phenylpyridin-2-yl]phenol 18.6% inhibition at 0.1 mM Homo sapiens
camptothecin
-
 Homo sapiens
additional information inhibitory activity, cytotoxicity, and structure-activity relationship study of hydroxylated 2,4-diphenyl-6-aryl pyridines, overview. Hydroxyl substitution at 3- or 3'-position of phenyl ring on 2,4-diphenyl-6-aryl pyridines might be required in order to show significant topo inhibitory activity. No inhibition by 15, 35, and 31 Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ required Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
commercial preparation recombinant topoisomerase I Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information relaxation of supercoiled pBR322 plasmid DNA Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
Topoisomerase I
-
 Homo sapiens

Temperature Optimum [°C]

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

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.9
-
 assay at Homo sapiens