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Literature summary for 5.6.2.2 extracted from

  • Pogorelcnik, B.; Janezic, M.; Sosic, I.; Gobec, S.; Solmajer, T.; Perdih, A.
    4,6-Substituted-1,3,5-triazin-2(1H)-ones as monocyclic catalytic inhibitors of human DNA topoisomerase IIalpha targeting the ATP binding site (2015), Bioorg. Med. Chem., 23, 4218-4229 .
    View publication on PubMed
Search for more literature for 5.6.2.2

Inhibitors

Inhibitors Comment Organism Structure
2-([[6-(benzylsulfanyl)-4-oxo-4,5-dihydro-1,3,5-triazin-2-yl]sulfanyl]methyl)benzonitrile
-
 Homo sapiens
3-([[6-(benzylsulfanyl)-4-oxo-4,5-dihydro-1,3,5-triazin-2-yl]sulfanyl]methyl)benzonitrile
-
 Homo sapiens
4-([[6-(benzylsulfanyl)-4-oxo-4,5-dihydro-1,3,5-triazin-2-yl]sulfanyl]methyl)-3-fluorobenzonitrile
-
 Homo sapiens
4-([[6-(benzylsulfanyl)-4-oxo-4,5-dihydro-1,3,5-triazin-2-yl]sulfanyl]methyl)benzonitrile
-
 Homo sapiens
6-(benzylsulfanyl)-4-(butylsulfanyl)-1,3,5-triazin-2(1H)-one
-
 Homo sapiens
6-(benzylsulfanyl)-4-(phenylsulfanyl)-1,3,5-triazin-2(1H)-one
-
 Homo sapiens
6-(benzylsulfanyl)-4-(propylsulfanyl)-1,3,5-triazin-2(1H)-one
-
 Homo sapiens
6-(benzylsulfanyl)-4-[(cyclobutylmethyl)sulfanyl]-1,3,5-triazin-2(1H)-one
-
 Homo sapiens
6-(benzylsulfanyl)-4-[(cyclopropylmethyl)sulfanyl]-1,3,5-triazin-2(1H)-one
-
 Homo sapiens
6-(benzylsulfanyl)-4-[[(2-chlorophenyl)methyl]sulfanyl]-1,3,5-triazin-2(1H)-one
-
 Homo sapiens
6-(benzylsulfanyl)-4-[[(2-fluorophenyl)methyl]sulfanyl]-1,3,5-triazin-2(1H)-one
-
 Homo sapiens
6-(benzylsulfanyl)-4-[[(2-methoxyphenyl)methyl]sulfanyl]-1,3,5-triazin-2(1H)-one
-
 Homo sapiens
6-(benzylsulfanyl)-4-[[(2-nitrophenyl)methyl]sulfanyl]-1,3,5-triazin-2(1H)-one
-
 Homo sapiens
6-(benzylsulfanyl)-4-[[(3-chlorophenyl)methyl]sulfanyl]-1,3,5-triazin-2(1H)-one
-
 Homo sapiens
6-(benzylsulfanyl)-4-[[(3-methoxyphenyl)methyl]sulfanyl]-1,3,5-triazin-2(1H)-one
-
 Homo sapiens
6-(benzylsulfanyl)-4-[[(3-nitrophenyl)methyl]sulfanyl]-1,3,5-triazin-2(1H)-one
-
 Homo sapiens
6-(benzylsulfanyl)-4-[[(4-chlorophenyl)methyl]sulfanyl]-1,3,5-triazin-2(1H)-one
-
 Homo sapiens
6-(benzylsulfanyl)-4-[[(4-fluorophenyl)methyl]sulfanyl]-1,3,5-triazin-2(1H)-one
-
 Homo sapiens
6-(benzylsulfanyl)-4-[[(4-nitrophenyl)methyl]sulfanyl]-1,3,5-triazin-2(1H)-one
-
 Homo sapiens
6-[(2-phenylethyl)sulfanyl]-9H-purin-2-amine
-
 Homo sapiens
9-(4-hydroxy-3,5-dimethoxyphenyl)-8-oxo-5,5a,6,8,8a,9-hexahydro-2H-furo[3',4':6,7]naphtho[2,3-d][1,3]dioxol-5-yl 4,6-O-ethylidenehexopyranoside
-
 Homo sapiens
ICRF-193
-
 Homo sapiens
N2-(1,3-benzothiazol-6-yl)-N6-tert-butyl-9H-purine-2,6-diamine
-
 Homo sapiens
N2-(4-fluorophenyl)-6-[[(1H-1,2,4-triazol-5-yl)sulfanyl]methyl]-1,3,5-triazine-2,4-diamine
-
 Homo sapiens
N6-tert-butyl-8-ethyl-N2-[2-[2-(morpholin-4-yl)ethoxy]quinolin-6-yl]-5,9-dihydro-4H-purine-2,6-diamine
-
 Homo sapiens
S-[6-(benzylsulfanyl)-4-oxo-4,5-dihydro-1,3,5-triazin-2-yl] hydrogen carbonothioate
-
 Homo sapiens
[4-amino-6-(4-fluoroanilino)-1,3,5-triazin-2-yl]methyl morpholine-4-carbodithioate
-
 Homo sapiens
[4-amino-6-(4-methoxyanilino)-1,3,5-triazin-2-yl]methyl morpholine-4-carbodithioate
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + relaxed pBR322 DNA
-
 Homo sapiens ADP + phosphate + supercoiled pBR322 DNA
-
 ?
ATP + supercoiled plasmid pNO1
-
 Homo sapiens ADP + phosphate + relaxed plasmid pNO1
-
 ?

Synonyms

Synonyms Comment Organism
DNA topoisomerase IIalpha
-
 Homo sapiens
tIIalpha
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0576
-
 at pH 7.9 and 37°C Homo sapiens 6-(benzylsulfanyl)-4-[[(3-chlorophenyl)methyl]sulfanyl]-1,3,5-triazin-2(1H)-one
0.0725
-
 at pH 7.9 and 37°C Homo sapiens 6-(benzylsulfanyl)-4-[[(2-fluorophenyl)methyl]sulfanyl]-1,3,5-triazin-2(1H)-one
0.0941
-
 at pH 7.9 and 37°C Homo sapiens 6-(benzylsulfanyl)-4-[[(2-chlorophenyl)methyl]sulfanyl]-1,3,5-triazin-2(1H)-one
0.1466
-
 at pH 7.9 and 37°C Homo sapiens 6-(benzylsulfanyl)-4-[[(4-fluorophenyl)methyl]sulfanyl]-1,3,5-triazin-2(1H)-one
0.1534
-
 at pH 7.9 and 37°C Homo sapiens 4-([[6-(benzylsulfanyl)-4-oxo-4,5-dihydro-1,3,5-triazin-2-yl]sulfanyl]methyl)benzonitrile
0.2193
-
 at pH 7.9 and 37°C Homo sapiens 6-(benzylsulfanyl)-4-[[(4-chlorophenyl)methyl]sulfanyl]-1,3,5-triazin-2(1H)-one
0.2347
-
 at pH 7.9 and 37°C Homo sapiens 6-(benzylsulfanyl)-4-(butylsulfanyl)-1,3,5-triazin-2(1H)-one
0.3767
-
 at pH 7.9 and 37°C Homo sapiens 6-(benzylsulfanyl)-4-[[(2-nitrophenyl)methyl]sulfanyl]-1,3,5-triazin-2(1H)-one
0.3859
-
 at pH 7.9 and 37°C Homo sapiens 6-(benzylsulfanyl)-4-[[(4-nitrophenyl)methyl]sulfanyl]-1,3,5-triazin-2(1H)-one
0.481
-
 at pH 7.9 and 37°C Homo sapiens 6-(benzylsulfanyl)-4-[(cyclopropylmethyl)sulfanyl]-1,3,5-triazin-2(1H)-one
0.4853
-
 at pH 7.9 and 37°C Homo sapiens 6-(benzylsulfanyl)-4-[[(3-methoxyphenyl)methyl]sulfanyl]-1,3,5-triazin-2(1H)-one
0.4858
-
 at pH 7.9 and 37°C Homo sapiens 4-([[6-(benzylsulfanyl)-4-oxo-4,5-dihydro-1,3,5-triazin-2-yl]sulfanyl]methyl)-3-fluorobenzonitrile
0.4883
-
 at pH 7.9 and 37°C Homo sapiens 6-(benzylsulfanyl)-4-[[(3-nitrophenyl)methyl]sulfanyl]-1,3,5-triazin-2(1H)-one
0.522
-
 at pH 7.9 and 37°C Homo sapiens 2-([[6-(benzylsulfanyl)-4-oxo-4,5-dihydro-1,3,5-triazin-2-yl]sulfanyl]methyl)benzonitrile
0.528
-
 at pH 7.9 and 37°C Homo sapiens 3-([[6-(benzylsulfanyl)-4-oxo-4,5-dihydro-1,3,5-triazin-2-yl]sulfanyl]methyl)benzonitrile
1
-
 at pH 7.9 and 37°C Homo sapiens 6-(benzylsulfanyl)-4-(phenylsulfanyl)-1,3,5-triazin-2(1H)-one
1
-
 at pH 7.9 and 37°C Homo sapiens 6-(benzylsulfanyl)-4-(propylsulfanyl)-1,3,5-triazin-2(1H)-one
1
-
 at pH 7.9 and 37°C Homo sapiens 6-(benzylsulfanyl)-4-[(cyclobutylmethyl)sulfanyl]-1,3,5-triazin-2(1H)-one
1
-
 at pH 7.9 and 37°C Homo sapiens S-[6-(benzylsulfanyl)-4-oxo-4,5-dihydro-1,3,5-triazin-2-yl] hydrogen carbonothioate
1
-
 IC50 above 1.0 mM, at pH 7.9 and 37°C Homo sapiens 6-(benzylsulfanyl)-4-[[(2-methoxyphenyl)methyl]sulfanyl]-1,3,5-triazin-2(1H)-one