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Literature summary for 5.6.2.1 extracted from

  • Ranjan, N.; Story, S.; Fulcrand, G.; Leng, F.; Ahmad, M.; King, A.; Sur, S.; Wang, W.; Tse-Dinh, Y.C.; Arya, D.P.
    Selective inhibition of Escherichia coli RNA and DNA topoisomerase I by Hoechst 33258 derived mono- and bisbenzimidazoles (2017), J. Med. Chem., 60, 4904-4922 .
    View publication on PubMed
Search for more literature for 5.6.2.1

Inhibitors

Inhibitors Comment Organism Structure
2'-(4-(3,6,9,12,15,18-hexaoxahenicos-20-ynyloxy)phenyl)-6-(4-methylpiperazin-1-yl)-1H,3'H-2,5'-bibenzo[d]imidazole
-
 Escherichia coli
2'-(4-(3,6,9,12,15,18-hexaoxahenicos-20-ynyloxy)phenyl)-6-(4-methylpiperazin-1-yl)-1H,3'H-2,5'-bibenzo[d]imidazole
-
 Homo sapiens
2'-[4-([6-[(but-3-yn-1-yl)oxy]hexyl]oxy)phenyl]-6-(4-methylpiperazin-1-yl)-1H,3'H-2,5'-bibenzimidazole
-
 Escherichia coli
2'-[4-([6-[(but-3-yn-1-yl)oxy]hexyl]oxy)phenyl]-6-(4-methylpiperazin-1-yl)-1H,3'H-2,5'-bibenzimidazole
-
 Homo sapiens
2'-[4-[(but-3-yn-1-yl)oxy]phenyl]-6-(4-methylpiperazin-1-yl)-1H,3'H-2,5'-bibenzimidazole
-
 Escherichia coli
2'-[4-[(but-3-yn-1-yl)oxy]phenyl]-6-(4-methylpiperazin-1-yl)-1H,3'H-2,5'-bibenzimidazole
-
 Homo sapiens
2'-[4-[(heptadec-16-yn-1-yl)oxy]phenyl]-6-(4-methylpiperazin-1-yl)-1H,3'H-2,5'-bibenzimidazole
-
 Escherichia coli
2'-[4-[(heptadec-16-yn-1-yl)oxy]phenyl]-6-(4-methylpiperazin-1-yl)-1H,3'H-2,5'-bibenzimidazole
-
 Homo sapiens
2'-[4-[(hex-5-yn-1-yl)oxy]phenyl]-6-(4-methylpiperazin-1-yl)-1H,3'H-2,5'-bibenzimidazole
-
 Escherichia coli
2'-[4-[(hex-5-yn-1-yl)oxy]phenyl]-6-(4-methylpiperazin-1-yl)-1H,3'H-2,5'-bibenzimidazole
-
 Homo sapiens
2-(4-((1-(2-azidoethyl)-1H-1,2,3-triazol-4-yl)methoxy)-phenyl)-6-(4-methylpiperazin-1-yl)-1H-benzo[d]imidazole
-
 Escherichia coli
2-(4-((1-(2-azidoethyl)-1H-1,2,3-triazol-4-yl)methoxy)-phenyl)-6-(4-methylpiperazin-1-yl)-1H-benzo[d]imidazole
-
 Homo sapiens
2-(4-(2-(4-(4-ethynylphenyl)-1H-1,2,3-triazol-1-yl)ethoxy)-phenyl)-6-(4-methylpiperazin-1-yl)-1H-benzo[d]imidazole
-
 Escherichia coli
2-(4-(2-(4-(4-ethynylphenyl)-1H-1,2,3-triazol-1-yl)ethoxy)-phenyl)-6-(4-methylpiperazin-1-yl)-1H-benzo[d]imidazole
-
 Homo sapiens
2-(4-ethoxyphenyl)-6-(4-methylpiperazin-1-yl)-1H-benzo[d]-imidazole
-
 Escherichia coli
2-(4-ethoxyphenyl)-6-(4-methylpiperazin-1-yl)-1H-benzo[d]-imidazole
-
 Homo sapiens
2-(4-hydroxyphenyl)-6-(4-methylpiperazin-1-yl)-1H-benzo-[d]imidazole-4-carboxylic acid
-
 Escherichia coli
2-(4-hydroxyphenyl)-6-(4-methylpiperazin-1-yl)-1H-benzo-[d]imidazole-4-carboxylic acid
-
 Homo sapiens
2-(4-[[1-(6-azidohexyl)-1H-1,2,3-triazol-4-yl]methoxy]phenyl)-6-(4-methylpiperazin-1-yl)-1H-benzimidazole
-
 Escherichia coli
2-(4-[[1-(6-azidohexyl)-1H-1,2,3-triazol-4-yl]methoxy]phenyl)-6-(4-methylpiperazin-1-yl)-1H-benzimidazole
-
 Homo sapiens
2-[4-(2-azidoethoxy)phenyl]-6-(4-methylpiperazin-1-yl)-1H-benzimidazole
-
 Escherichia coli
2-[4-(2-azidoethoxy)phenyl]-6-(4-methylpiperazin-1-yl)-1H-benzimidazole
-
 Homo sapiens
3-(4-(6-(4-methylpiperazin-1-yl)-1H-benzo[d]imidazol-2-yl)-phenoxy)propan-1-amine
-
 Escherichia coli
3-(4-(6-(4-methylpiperazin-1-yl)-1H-benzo[d]imidazol-2-yl)-phenoxy)propan-1-amine
-
 Homo sapiens
4-(1H-benzo[d]imidazol-2-yl)phenol
-
 Escherichia coli
4-(1H-benzo[d]imidazol-2-yl)phenol
-
 Homo sapiens
5-(4-methylpiperazin-1-yl)-2-(4-(6-(prop-2-ynyloxy)-hexyloxy)phenyl)-1H-benzo[d]imidazole
-
 Escherichia coli
5-(4-methylpiperazin-1-yl)-2-(4-(6-(prop-2-ynyloxy)-hexyloxy)phenyl)-1H-benzo[d]imidazole
-
 Homo sapiens
6-(4-methylpiperazin-1-yl)-2'-(4-(10-(prop-2-ynyloxy)-decyloxy)phenyl)-1H,3'H-2,5'-bibenzo[d]imidazole
-
 Escherichia coli
6-(4-methylpiperazin-1-yl)-2'-(4-(10-(prop-2-ynyloxy)-decyloxy)phenyl)-1H,3'H-2,5'-bibenzo[d]imidazole
-
 Homo sapiens
6-(4-methylpiperazin-1-yl)-2'-(4-(12-(prop-2-ynyloxy)-dodecyloxy)phenyl)-1H,3'H-2,5'-bibenzo[d]imidazole
-
 Escherichia coli
6-(4-methylpiperazin-1-yl)-2'-(4-(12-(prop-2-ynyloxy)-dodecyloxy)phenyl)-1H,3'H-2,5'-bibenzo[d]imidazole
-
 Homo sapiens
6-(4-methylpiperazin-1-yl)-2'-(4-(6-(prop-2-ynyloxy)-hexyloxy)phenyl)-1H,3'H-2,5'-bibenzo[d]imidazole
-
 Escherichia coli
6-(4-methylpiperazin-1-yl)-2'-(4-(6-(prop-2-ynyloxy)-hexyloxy)phenyl)-1H,3'H-2,5'-bibenzo[d]imidazole
-
 Homo sapiens
6-(4-methylpiperazin-1-yl)-2'-(4-(8-(prop-2-ynyloxy)-octyloxy)phenyl)-1H,3'H-2,5'-bibenzo[d]imidazole
-
 Escherichia coli
6-(4-methylpiperazin-1-yl)-2'-(4-(8-(prop-2-ynyloxy)-octyloxy)phenyl)-1H,3'H-2,5'-bibenzo[d]imidazole
-
 Homo sapiens
6-(4-methylpiperazin-1-yl)-2-(4-(2-(4-(oct-7-ynyl)-1H-1,2,3-triazol-1-yl)ethoxy)phenyl)-1H-benzo[d]imidazole
-
 Escherichia coli
6-(4-methylpiperazin-1-yl)-2-(4-(2-(4-(oct-7-ynyl)-1H-1,2,3-triazol-1-yl)ethoxy)phenyl)-1H-benzo[d]imidazole
-
 Homo sapiens
6-(4-methylpiperazin-1-yl)-2-[4-[(prop-2-yn-1-yl)oxy]phenyl]-1H-benzimidazole
-
 Escherichia coli
6-(4-methylpiperazin-1-yl)-2-[4-[(prop-2-yn-1-yl)oxy]phenyl]-1H-benzimidazole
-
 Homo sapiens
Hoechst 33258
-
 Escherichia coli
Hoechst 33258
-
 Homo sapiens
Hoechst 33342
-
 Escherichia coli
Hoechst 33342
-
 Homo sapiens
methyl 2-(4-Hydroxyphenyl)-6-(4-methylpiperazin-1-yl)-1H-benzo[d]imidazole-4-carboxylate
-
 Escherichia coli
methyl 2-(4-Hydroxyphenyl)-6-(4-methylpiperazin-1-yl)-1H-benzo[d]imidazole-4-carboxylate
-
 Homo sapiens
tert-butyl 3-(4-(6-(4-methylpiperazin-1-yl)-1H-benzo[d]-imidazol-2-yl)phenoxy)propylcarbamate
-
 Escherichia coli
tert-butyl 3-(4-(6-(4-methylpiperazin-1-yl)-1H-benzo[d]-imidazol-2-yl)phenoxy)propylcarbamate
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Escherichia coli
-
-
-
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
supercoiled plasmid pBAD-GFPuv
-
 Escherichia coli ?
-
 ?
supercoiled plasmid pBAD-GFPuv
-
 Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
DNA topoisomerase I
-
 Escherichia coli
DNA topoisomerase I
-
 Homo sapiens
topoI
-
 Escherichia coli
topoI
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00247
-
 pH and temperature not specified in the publication Escherichia coli 2'-[4-[(heptadec-16-yn-1-yl)oxy]phenyl]-6-(4-methylpiperazin-1-yl)-1H,3'H-2,5'-bibenzimidazole
0.0028
-
 pH and temperature not specified in the publication Escherichia coli 6-(4-methylpiperazin-1-yl)-2'-(4-(8-(prop-2-ynyloxy)-octyloxy)phenyl)-1H,3'H-2,5'-bibenzo[d]imidazole
0.0032
-
 pH and temperature not specified in the publication Escherichia coli 6-(4-methylpiperazin-1-yl)-2'-(4-(6-(prop-2-ynyloxy)-hexyloxy)phenyl)-1H,3'H-2,5'-bibenzo[d]imidazole
0.004
-
 pH and temperature not specified in the publication Escherichia coli 6-(4-methylpiperazin-1-yl)-2'-(4-(12-(prop-2-ynyloxy)-dodecyloxy)phenyl)-1H,3'H-2,5'-bibenzo[d]imidazole
0.00457
-
 pH and temperature not specified in the publication Escherichia coli 2'-[4-[(hex-5-yn-1-yl)oxy]phenyl]-6-(4-methylpiperazin-1-yl)-1H,3'H-2,5'-bibenzimidazole
0.005
-
 IC50 above 0.05 mM, at pH 7.9 and 37°C Homo sapiens Hoechst 33342
0.0055
-
 pH and temperature not specified in the publication Escherichia coli 2'-[4-[(but-3-yn-1-yl)oxy]phenyl]-6-(4-methylpiperazin-1-yl)-1H,3'H-2,5'-bibenzimidazole
0.00663
-
 pH and temperature not specified in the publication Escherichia coli 2'-[4-([6-[(but-3-yn-1-yl)oxy]hexyl]oxy)phenyl]-6-(4-methylpiperazin-1-yl)-1H,3'H-2,5'-bibenzimidazole
0.01224
-
 pH and temperature not specified in the publication Escherichia coli 6-(4-methylpiperazin-1-yl)-2'-(4-(10-(prop-2-ynyloxy)-decyloxy)phenyl)-1H,3'H-2,5'-bibenzo[d]imidazole
0.0195
-
 at pH 7.9 and 37°C Escherichia coli Hoechst 33258
0.0215
-
 pH and temperature not specified in the publication Escherichia coli 2-(4-[[1-(6-azidohexyl)-1H-1,2,3-triazol-4-yl]methoxy]phenyl)-6-(4-methylpiperazin-1-yl)-1H-benzimidazole
0.02286
-
 at pH 7.9 and 37°C Homo sapiens Hoechst 33258
0.02983
-
 at pH 7.9 and 37°C Escherichia coli Hoechst 33342
0.05
-
 IC50 above 0.05 mM, pH and temperature not specified in the publication Escherichia coli 2'-(4-(3,6,9,12,15,18-hexaoxahenicos-20-ynyloxy)phenyl)-6-(4-methylpiperazin-1-yl)-1H,3'H-2,5'-bibenzo[d]imidazole
0.05
-
 IC50 above 0.05 mM, pH and temperature not specified in the publication Homo sapiens 2'-[4-[(hex-5-yn-1-yl)oxy]phenyl]-6-(4-methylpiperazin-1-yl)-1H,3'H-2,5'-bibenzimidazole
0.05
-
 IC50 above 0.05 mM, pH and temperature not specified in the publication Homo sapiens 6-(4-methylpiperazin-1-yl)-2'-(4-(10-(prop-2-ynyloxy)-decyloxy)phenyl)-1H,3'H-2,5'-bibenzo[d]imidazole
0.05
-
 IC50 above 0.05 mM, pH and temperature not specified in the publication Homo sapiens 6-(4-methylpiperazin-1-yl)-2'-(4-(12-(prop-2-ynyloxy)-dodecyloxy)phenyl)-1H,3'H-2,5'-bibenzo[d]imidazole
0.05
-
 IC50 above 0.05 mM, pH and temperature not specified in the publication Homo sapiens 6-(4-methylpiperazin-1-yl)-2'-(4-(6-(prop-2-ynyloxy)-hexyloxy)phenyl)-1H,3'H-2,5'-bibenzo[d]imidazole
0.05
-
 IC50 above 0.05 mM, pH and temperature not specified in the publication Homo sapiens 6-(4-methylpiperazin-1-yl)-2'-(4-(8-(prop-2-ynyloxy)-octyloxy)phenyl)-1H,3'H-2,5'-bibenzo[d]imidazole
0.05
-
 IC50 above 0.05 mM, pH and temperature not specified in the publication Homo sapiens 2'-[4-([6-[(but-3-yn-1-yl)oxy]hexyl]oxy)phenyl]-6-(4-methylpiperazin-1-yl)-1H,3'H-2,5'-bibenzimidazole
0.05
-
 IC50 above 0.05 mM, pH and temperature not specified in the publication Homo sapiens 2'-[4-[(heptadec-16-yn-1-yl)oxy]phenyl]-6-(4-methylpiperazin-1-yl)-1H,3'H-2,5'-bibenzimidazole
0.05
-
 IC50 above 0.05 mM, pH and temperature not specified in the publication Homo sapiens 2-(4-[[1-(6-azidohexyl)-1H-1,2,3-triazol-4-yl]methoxy]phenyl)-6-(4-methylpiperazin-1-yl)-1H-benzimidazole
0.2541
-
 pH and temperature not specified in the publication Homo sapiens 2'-[4-[(but-3-yn-1-yl)oxy]phenyl]-6-(4-methylpiperazin-1-yl)-1H,3'H-2,5'-bibenzimidazole