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Literature summary for 5.6.2.2 extracted from

  • Yao, B.L.; Mai, Y.W.; Chen, S.B.; Xie, H.T.; Yao, P.F.; Ou, T.M.; Tan, J.H.; Wang, H.G.; Li, D.; Huang, S.L.; Gu, L.Q.; Huang, Z.S.
    Design, synthesis and biological evaluation of novel 7-alkylamino substituted benzo[a]phenazin derivatives as dual topoisomerase I/II inhibitors (2015), Eur. J. Med. Chem., 92, 540-553 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
1,4-Naphthoquinone
-
Homo sapiens
10-chloro-7-(3-(dimethylamino)propyl)-3-methoxybenzo[a]phenazin-5(7H)- one
-
Homo sapiens
10-chloro-7-(3-(dimethylamino)propyl)benzo[a]phenazin-5(7H)-one
-
Homo sapiens
3-[(10-methoxybenzo[a]phenazin-5-yl)oxy]-N,N-dimethylpropan-1-amine
-
Homo sapiens
7-(2-(4-methylpiperazin-1-yl)ethyl)benzo[a]phenazin-5(7H)-one
-
Homo sapiens
7-(2-(diethylamino)ethyl)benzo[a]phenazin-5(7H)-one
-
Homo sapiens
7-(2-(dimethylamino)ethyl)-3-methoxybenzo[a]phenazin-5(7H)-one
-
Homo sapiens
7-(2-(dimethylamino)ethyl)benzo[a]phenazin-5(7H)-one
-
Homo sapiens
7-(2-(piperidin-1-yl)ethyl)benzo[a]phenazin-5(7H)-one
-
Homo sapiens
7-(2-morpholinoethyl)benzo[a]phenazin-5(7H)-one
-
Homo sapiens
7-(3-(4-methylpiperazin-1-yl)propyl)benzo[a]phenazin-5(7H)-one
-
Homo sapiens
7-(3-(diethylamino)propyl)-3-methoxybenzo[a]phenazin-5(7H)-one
-
Homo sapiens
7-(3-(diethylamino)propyl)benzo[a]phenazin-5(7H)-one
-
Homo sapiens
7-(3-(dimethylamino)propyl)-10-methoxybenzo[a]phenazin-5(7H)-one
-
Homo sapiens
7-(3-(dimethylamino)propyl)-2-methoxybenzo[a]phenazin-5(7H)-one
-
Homo sapiens
7-(3-(dimethylamino)propyl)-3,10-dimethoxybenzo[a]phenazin-5(7H)-one
-
Homo sapiens
7-(3-(dimethylamino)propyl)-3,9-dimethoxybenzo[a]phenazin-5(7H)-one
-
Homo sapiens
7-(3-(dimethylamino)propyl)-3-methoxybenzo[a]phenazin-5(7H)-one
-
Homo sapiens
7-(3-(dimethylamino)propyl)-9-methoxybenzo[a]phenazin-5(7H)-one
-
Homo sapiens
7-(3-(dimethylamino)propyl)benzo[a]phenazin-5(7H)-one
-
Homo sapiens
7-(3-(dimethylamino)propyl)benzo[f]pyrido[2,3-b]quinoxalin-5(7H)-one
-
Homo sapiens
7-(3-(piperidin-1-yl)propyl)benzo[a]phenazin-5(7H)-one
-
Homo sapiens
7-(3-(piperidin-1-yl)propyl)benzo[f]pyrido[2,3-b]quinoxalin-5(7H)-one
-
Homo sapiens
7-(3-(pyrrolidin-1-yl)propyl)benzo[a]phenazin-5(7H)-one
-
Homo sapiens
7-(3-morpholinopropyl)benzo[a]phenazin-5(7H)-one
-
Homo sapiens
7-(4-(diethylamino)butyl)benzo[a]phenazin-5(7H)-one
-
Homo sapiens
7-(4-(dimethylamino)butyl)benzo[a]phenazin-5(7H)-one
-
Homo sapiens
7-propylbenzo[a]phenazin-5(7H)-one
-
Homo sapiens
benzo[a]phenazine
-
Homo sapiens
camptothecin
-
Homo sapiens
NC-190
-
Homo sapiens
VP-16
-
Homo sapiens
XR 11576
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P11388
-
-

Source Tissue

Source Tissue Comment Organism Textmining
A-549 cell
-
Homo sapiens
-
HeLa cell
-
Homo sapiens
-
HL-60 cell
-
Homo sapiens
-
K-562 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
topo II
-
Homo sapiens
Topoisomerase II
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00006
-
enzyme from HL-60 cell, at pH 8.0 and 37°C Homo sapiens VP-16
0.00007
-
enzyme from HL-60 cell, at pH 8.0 and 37°C Homo sapiens camptothecin
0.00054
-
enzyme from HeLa cell, at pH 8.0 and 37°C Homo sapiens VP-16
0.00164
-
enzyme from K-562 cell, at pH 8.0 and 37°C Homo sapiens VP-16
0.00537
-
enzyme from K-562 cell, at pH 8.0 and 37°C Homo sapiens camptothecin
0.00891
-
enzyme from A-549 cell, at pH 8.0 and 37°C Homo sapiens VP-16
0.01162
-
enzyme from HeLa cell, at pH 8.0 and 37°C Homo sapiens camptothecin
0.02645
-
enzyme from A-549 cell, at pH 8.0 and 37°C Homo sapiens camptothecin