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Literature summary for 5.6.2.2 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

Inhibitors

Inhibitors Comment Organism Structure
2,2'-(4-phenylpyridine-2,6-diyl)diphenol 42.7% inhibition at 0.1 mM Homo sapiens
2-(2,6-diphenylpyridin-4-yl)phenol
-
Homo sapiens
2-(4,6-diphenylpyridin-2-yl)phenol
-
Homo sapiens
2-(4-phenyl-2,2'-bipyridin-6-yl)phenol
-
Homo sapiens
2-(4-phenyl-2,3'-bipyridin-6-yl)phenol
-
Homo sapiens
2-(4-phenyl-2,4'-bipyridin-6-yl)phenol
-
Homo sapiens
2-(6-phenyl-2,2'-bipyridin-4-yl)phenol
-
Homo sapiens
2-(6-phenyl-2,3'-bipyridin-4-yl)phenol
-
Homo sapiens
2-(6-phenyl-2,4'-bipyridin-4-yl)phenol
-
Homo sapiens
2-[4-phenyl-6-(thiophen-2-yl)pyridin-2-yl]phenol
-
Homo sapiens
2-[4-phenyl-6-(thiophen-3-yl)pyridin-2-yl]phenol
-
Homo sapiens
2-[6-(furan-2-yl)-4-phenylpyridin-2-yl]phenol
-
Homo sapiens
3,3'-(4-phenylpyridine-2,6-diyl)diphenol 86.5% inhibition at 0.1 mM Homo sapiens
3-(2,6-diphenylpyridin-4-yl)phenol 68.2% inhibition at 0.1 mM Homo sapiens
3-(4,6-diphenylpyridin-2-yl)phenol 48.4% inhibition at 0.1 mM Homo sapiens
3-(4-phenyl-2,2'-bipyridin-6-yl)phenol
-
Homo sapiens
3-(4-phenyl-2,3'-bipyridin-6-yl)phenol
-
Homo sapiens
3-(4-phenyl-2,4'-bipyridin-6-yl)phenol 3.6% inhibition at 0.1 mM Homo sapiens
3-(6-phenyl-2,2'-bipyridin-4-yl)phenol 48.1% inhibition at 0.1 mM Homo sapiens
3-(6-phenyl-2,3'-bipyridin-4-yl)phenol 37.1% inhibition at 0.1 mM Homo sapiens
3-(6-phenyl-2,4'-bipyridin-4-yl)phenol 42.8% inhibition at 0.1 mM Homo sapiens
3-[2-(furan-2-yl)-6-phenylpyridin-4-yl]phenol 47.5% inhibition at 0.1 mM Homo sapiens
3-[2-phenyl-6-(thiophen-2-yl)pyridin-4-yl]phenol 57.5% inhibition at 0.1 mM Homo sapiens
3-[2-phenyl-6-(thiophen-3-yl)pyridin-4-yl]phenol 52.6% inhibition at 0.1 mM Homo sapiens
3-[4-phenyl-6-(thiophen-2-yl)pyridin-2-yl]phenol 53.8% inhibition at 0.1 mM Homo sapiens
3-[4-phenyl-6-(thiophen-3-yl)pyridin-2-yl]phenol 51.8% inhibition at 0.1 mM Homo sapiens
3-[6-(furan-2-yl)-4-phenylpyridin-2-yl]phenol 51.6% inhibition at 0.1 mM Homo sapiens
4,4'-(4-phenylpyridine-2,6-diyl)diphenol 76.8% inhibition at 0.1 mM Homo sapiens
4-(2,6-diphenylpyridin-4-yl)phenol
-
Homo sapiens
4-(4,6-diphenylpyridin-2-yl)phenol 27.6% inhibition at 0.1 mM Homo sapiens
4-(4-phenyl-2,2'-bipyridin-6-yl)phenol
-
Homo sapiens
4-(4-phenyl-2,3'-bipyridin-6-yl)phenol 18.6% inhibition at 0.1 mM Homo sapiens
4-(4-phenyl-2,4'-bipyridin-6-yl)phenol
-
Homo sapiens
4-(6-phenyl-2,2'-bipyridin-4-yl)phenol
-
Homo sapiens
4-(6-phenyl-2,3'-bipyridin-4-yl)phenol
-
Homo sapiens
4-(6-phenyl-2,4'-bipyridin-4-yl)phenol 8.4% inhibition at 0.1 mM Homo sapiens
4-[2-(furan-2-yl)-6-phenylpyridin-4-yl]phenol 30.2% inhibition at 0.1 mM Homo sapiens
4-[2-phenyl-6-(thiophen-2-yl)pyridin-4-yl]phenol
-
Homo sapiens
4-[2-phenyl-6-(thiophen-3-yl)pyridin-4-yl]phenol
-
Homo sapiens
4-[4-phenyl-6-(thiophen-2-yl)pyridin-2-yl]phenol 35.4% inhibition at 0.1 mM Homo sapiens
4-[4-phenyl-6-(thiophen-3-yl)pyridin-2-yl]phenol 38.3% inhibition at 0.1 mM Homo sapiens
4-[6-(furan-2-yl)-4-phenylpyridin-2-yl]phenol 35.2% inhibition at 0.1 mM Homo sapiens
additional information synthesis, topoisomerase IIalpha inhibitory activity, cytotoxicity in human cancer cell lines, 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 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information cleavage of negatively supercoiled pBR322 plasmid DNA by topoisomerase IIalpha Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
DNA topoisomerase IIalpha
-
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