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Literature summary for 5.6.2.1 extracted from

  • Shi, W.; Marcus, S.L.; Lowary, T.L.
    Cytotoxicity and topoisomerase I/II inhibition of glycosylated 2-phenyl-indoles, 2-phenyl-benzo[b]thiophenes and 2-phenyl-benzo[b]furans (2011), Bioorg. Med. Chem., 19, 603-612.
    View publication on PubMed
Search for more literature for 5.6.2.1

Inhibitors

Inhibitors Comment Organism Structure
(2S,3R,4S,6R)-4-amino-2-methyl-6-((3-(2-phenyl-1-tosyl-1H-indol-3-yl)prop-2-yn-1-yl)oxy)tetrahydro-2H-pyran-3-ol 92.8% inhibition at 0.1 mM Homo sapiens
(2S,3R,4S,6R)-4-amino-2-methyl-6-((3-(2-phenylbenzofuran-3-yl)prop-2-yn-1-yl)oxy)tetrahydro-2H-pyran-3-ol 25.5% inhibition at 0.1 mM Homo sapiens
(2S,3R,4S,6R)-4-amino-2-methyl-6-((3-(2-phenylbenzo[b]thiophen-3-yl)prop-2-yn-1-yl)oxy)tetrahydro-2H-pyran-3-ol 32.2% inhibition at 0.1 mM Homo sapiens
(2S,3R,4S,6R)-4-amino-2-methyl-6-(3-(2-phenyl-1H-indol-3-yl)prop-2-ynyloxy)tetrahydro-2H-pyran-3-ol 20.2% inhibition at 0.1 mM; 8.2% inhibition at 0.1 mM Homo sapiens
(2S,3S,6R)-2-methyl-6-(3-(2-phenyl-1-tosyl-1H-indol-3-yl)prop-2-ynyloxy)tetrahydro-2H-pyran-3-amine 43.2% inhibition at 0.1 mM Homo sapiens
(2S,3S,6R)-2-methyl-6-(3-(2-phenyl-1H-indol-3-yl)prop-2-ynyloxy)tetrahydro-2H-pyran-3-amine 4.0% inhibition at 0.1 mM Homo sapiens
(2S,3S,6R)-2-methyl-6-(3-(2-phenylbenzo[b]thiophen-3-yl)prop-2-ynyloxy)tetrahydro-2H-pyran-3-amine 7.9% inhibition at 0.1 mM Homo sapiens
3-(2-phenyl-1-benzofuran-3-yl)prop-2-yn-1-yl 3-amino-2,3,6-trideoxy-b-D-arabino-hexopyranoside 77.8% inhibition at 0.1 mM Homo sapiens
3-(2-phenyl-1-benzothiophen-3-yl)prop-2-yn-1-yl 3-amino-2,3,6-trideoxy-b-D-arabino-hexopyranoside 36.9% inhibition at 0.1 mM Homo sapiens
3-(2-phenyl-1H-indol-3-yl)prop-2-yn-1-yl 3-amino-2,3,6-trideoxy-b-D-arabino-hexopyranoside 8.8% inhibition at 0.1 mM Homo sapiens
3-[1-[(4-methylphenyl)sulfonyl]-2-phenyl-1H-indol-3-yl]prop-2-yn-1-yl 3-amino-2,3,6-trideoxy-b-D-arabino-hexopyranoside 80.1% inhibition at 0.1 mM Homo sapiens
additional information topoisomerase I inhibition of glycosylated 2-phenyl-indoles, 2-phenyl-benzo[b]thiophenes and 2-phenyl-benzo[b]furans, overview. Analysis of cytotoxocity against three human non-tumor cell lines analyzed by the MTS (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium) cell viability assay Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
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-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information cleavage of supercoiled DNA by topoisomerase I Homo sapiens ?
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 ?

Synonyms

Synonyms Comment Organism
Topo I
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 Homo sapiens
Topoisomerase I
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 Homo sapiens

Temperature Optimum [°C]

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