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Literature summary for 5.6.2.2 extracted from

  • Baviskar, A.T.; Madaan, C.; Preet, R.; Mohapatra, P.; Jain, V.; Agarwal, A.; Guchhait, S.K.; Kundu, C.N.; Banerjee, U.C.; Bharatam, P.V.
    N-fused imidazoles as novel anticancer agents that inhibit catalytic activity of topoisomerase IIalpha and induce apoptosis in G1/S phase (2011), J. Med. Chem., 54, 5013-5030.
    View publication on PubMed
Search for more literature for 5.6.2.2

Inhibitors

Inhibitors Comment Organism Structure
2-(4-chlorophenyl)-N-cyclohexylimidazo[1,2-a]pyrazin-3-amine
-
 Homo sapiens
2-(4-chlorophenyl)imidazo[1,2-a]pyrazin-3-amine
-
 Homo sapiens
2-(4-chlorophenyl)imidazo[1,2-a]pyridin-3-amine
-
 Homo sapiens
2-(4-methoxyphenyl)imidazo[1,2-a]pyrazin-3-amine
-
 Homo sapiens
4-(3-amino-6-bromoimidazo[1,2-a]pyridin-2-yl)benzonitrile
-
 Homo sapiens
4-[2-(tert-butylamino)imidazo[1,2-a]pyrimidin-3-yl]benzonitrile
-
 Homo sapiens
4-[3-(tert-butylamino)imidazo[1,2-a]pyrazin-2-yl]benzoic acid
-
 Homo sapiens
4-[3-(tert-butylamino)imidazo[1,2-a]pyridin-2-yl]benzoic acid
-
 Homo sapiens
4-[3-(tert-butylamino)imidazo[1,2-a]pyridin-2-yl]benzonitrile
-
 Homo sapiens
6-chloro-2-(pyridin-2-yl)imidazo[1,2-a]pyridin-3-amine
-
 Homo sapiens
ethyl 2-(4-chlorophenyl)-3-(cyclohexylamino)-1H-imidazo[1,2-b]pyrazole-7-carboxylate
-
 Homo sapiens
ethyl 3-(tert-butylamino)-2-(4-chlorophenyl)-1H-imidazo[1,2-b]pyrazole-7-carboxylate
-
 Homo sapiens
ethyl 3-amino-2-(4-chlorophenyl)-1H-imidazo[1,2-b]pyrazole-7-carboxylate
-
 Homo sapiens
additional information structure-activity relationship study, molecular docking studies based on 5'-adenylyl-beta,gamma-imidodiphosphate-bound enzyme, PDB ID 1ZXM, and ADP-bound form, PDB 1ZXN, and molecular dynamics simulation analysis for design of structure-based inhibitors, overview. The catalytic mode of inhibition proceeds by blocking the ATP-binding site Homo sapiens
N-tert-butyl-2-(1H-pyrrol-2-yl)imidazo[1,2-a]pyridin-3-amine
-
 Homo sapiens
N-tert-butyl-2-(2-chlorophenyl)imidazo[1,2-a]pyrazin-3-amine
-
 Homo sapiens
N-tert-butyl-2-(3-methoxyphenyl)imidazo[1,2-a]pyrazin-3-amine
-
 Homo sapiens
N-tert-butyl-2-(4-chlorophenyl)-7-methylimidazo[1,2-a]pyridin-3-amine
-
 Homo sapiens
N-tert-butyl-2-(4-chlorophenyl)-9H-imidazo[1,2-a]benzimidazol-3-amine
-
 Homo sapiens
N-tert-butyl-2-(4-chlorophenyl)imidazo[1,2-a]pyrazin-3-amine
-
 Homo sapiens
N-tert-butyl-2-(4-chlorophenyl)imidazo[1,2-a]pyridin-3-amine
-
 Homo sapiens
N-tert-butyl-2-(4-chlorophenyl)imidazo[1,2-a]pyrimidin-3-amine
-
 Homo sapiens
N-tert-butyl-2-(naphthalen-1-yl)imidazo[1,2-a]pyridin-3-amine
-
 Homo sapiens
N-tert-butyl-2-(pyridin-2-yl)imidazo[1,2-a]pyridin-3-amine
-
 Homo sapiens
N-tert-butyl-2-phenylimidazo[1,2-a]pyrazin-3-amine
-
 Homo sapiens
N-tert-butyl-2-phenylimidazo[1,2-a]pyridin-3-amine
-
 Homo sapiens
N-tert-butyl-2-propylimidazo[1,2-a]pyridin-3-amine
-
 Homo sapiens
N-tert-butyl-2-[4-(dimethylamino)phenyl]imidazo[1,2-a]pyridin-3-amine
-
 Homo sapiens
N-tert-butyl-6-chloro-2-(4-chlorophenyl)imidazo[1,2-a]pyridin-3-amine
-
 Homo sapiens
N-tert-butyl-6-chloro-2-(4-fluorophenyl)imidazo[1,2-a]pyridin-3-amine
-
 Homo sapiens
N-tert-butylimidazo[1,2-a]pyrazin-3-amine
-
 Homo sapiens
N-tert-butylimidazo[1,2-a]pyridin-3-amine
-
 Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
nucleus
-
 Homo sapiens 5634
-

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ required Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P11388
-
-

Source Tissue

Source Tissue Comment Organism Textmining
HEK-293 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information kinetoplast DNA is used as a substrate in a decatenation assay Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
hTopoIIalpha
-
 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
7.5
-
 ATPase and topoisomerase inhibition assay at Homo sapiens
8
-
 TopoII-mediated DNA decatenation assay at Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP ATP and AMPPNP dock into the ATPase domain of hTopoIIalpha Homo sapiens
additional information binding structure of 5'-adenylyl-beta,gamma-imidodiphosphate, i.e AMPPNP, a nonhydrolyzable ATP analogue, PDB ID 1ZXM Homo sapiens