Literature summary for 5.6.2.2 extracted from

Huang, H.; Chen, Q.; Ku, X.; Meng, L.; Lin, L.; Wang, X.; Zhu, C.; Wang, Y.; Chen, Z.; Li, M.; Jiang, H.; Chen, K.; Ding, J.; Liu, H.
A series of alpha-heterocyclic carboxaldehyde thiosemicarbazones inhibit topoisomerase IIalpha catalytic activity (2010), J. Med. Chem., 53, 3048-3064.

Inhibitors

Inhibitors	Comment	Organism
(2E)-2-(1,3-benzothiazol-2-ylmethylidene)-N,N-dimethylhydrazinecarbothioamide	-	Homo sapiens
(2E)-2-(1,3-benzothiazol-2-ylmethylidene)hydrazinecarbothioamide	-	Homo sapiens
(2E)-2-(1,8-naphthyridin-2-ylmethylidene)hydrazinecarbothioamide	-	Homo sapiens
(2E)-2-(1-benzothiophen-2-ylmethylidene)hydrazinecarbothioamide	-	Homo sapiens
(2E)-2-(benzo[h][1,6]naphthyridin-5-ylmethylidene)-N,N-dimethylhydrazinecarbothioamide	-	Homo sapiens
(2E)-2-(benzo[h][1,6]naphthyridin-5-ylmethylidene)hydrazinecarbothioamide	-	Homo sapiens
(2E)-2-(quinolin-2-ylmethylidene)-N-[2-(trifluoromethyl)phenyl]hydrazinecarbothioamide	-	Homo sapiens
(2E)-2-(quinolin-2-ylmethylidene)-N-[4-(trifluoromethyl)phenyl]hydrazinecarbothioamide	-	Homo sapiens
(2E)-2-(quinolin-2-ylmethylidene)hydrazinecarbothioamide	-	Homo sapiens
(2E)-2-(quinoxalin-2-ylmethylidene)hydrazinecarbothioamide	-	Homo sapiens
(2E)-2-(thieno[2,3-b]pyridin-2-ylmethylidene)hydrazinecarbothioamide	-	Homo sapiens
(2E)-2-[(3,4-dimethylthieno[2,3-b]thiophen-2-yl)methylidene]hydrazinecarbothioamide	-	Homo sapiens
(2E)-N,N-dimethyl-2-(1,8-naphthyridin-2-ylmethylidene)hydrazinecarbothioamide	-	Homo sapiens
(2E)-N,N-dimethyl-2-(quinolin-2-ylmethylidene)hydrazinecarbothioamide	exhibits broad antiproliferative activity arresting synchronized cells at the M-phase, also exhibits iron chelator activity, and topoisomerase IIalpha catalytic inhibition, the latter due to direct interaction with the ATPase domain, blocks of ATP hydroly	Homo sapiens
(2E)-N,N-dimethyl-2-(quinoxalin-2-ylmethylidene)hydrazinecarbothioamide	-	Homo sapiens
(2E)-N,N-dimethyl-2-(thieno[2,3-b]pyridin-2-ylmethylidene)hydrazinecarbothioamide	-	Homo sapiens
(2E)-N-(2-bromophenyl)-2-(quinolin-2-ylmethylidene)hydrazinecarbothioamide	-	Homo sapiens
(2E)-N-(2-fluorophenyl)-2-(quinolin-2-ylmethylidene)hydrazinecarbothioamide	-	Homo sapiens
(2E)-N-(2-methoxy-5-methylphenyl)-2-(quinolin-2-ylmethylidene)hydrazinecarbothioamide	-	Homo sapiens
(2E)-N-(2-methoxyphenyl)-2-(quinolin-2-ylmethylidene)hydrazinecarbothioamide	-	Homo sapiens
(2E)-N-(2-methylphenyl)-2-(quinolin-2-ylmethylidene)hydrazinecarbothioamide	-	Homo sapiens
(2E)-N-(3-bromophenyl)-2-(quinolin-2-ylmethylidene)hydrazinecarbothioamide	-	Homo sapiens
(2E)-N-(3-chlorophenyl)-2-(quinolin-2-ylmethylidene)hydrazinecarbothioamide	-	Homo sapiens
(2E)-N-(3-fluorophenyl)-2-(quinolin-2-ylmethylidene)hydrazinecarbothioamide	-	Homo sapiens
(2E)-N-(3-methoxyphenyl)-2-(quinolin-2-ylmethylidene)hydrazinecarbothioamide	-	Homo sapiens
(2E)-N-(3-methylphenyl)-2-(quinolin-2-ylmethylidene)hydrazinecarbothioamide	-	Homo sapiens
(2E)-N-(4-bromophenyl)-2-(quinolin-2-ylmethylidene)hydrazinecarbothioamide	-	Homo sapiens
(2E)-N-(4-chlorophenyl)-2-(quinolin-2-ylmethylidene)hydrazinecarbothioamide	-	Homo sapiens
(2E)-N-(4-cyanophenyl)-2-(quinolin-2-ylmethylidene)hydrazinecarbothioamide	-	Homo sapiens
(2E)-N-(4-fluorophenyl)-2-(quinolin-2-ylmethylidene)hydrazinecarbothioamide	-	Homo sapiens
(2E)-N-(4-methoxyphenyl)-2-(quinolin-2-ylmethylidene)hydrazinecarbothioamide	-	Homo sapiens
(2E)-N-(4-methylphenyl)-2-(quinolin-2-ylmethylidene)hydrazinecarbothioamide	-	Homo sapiens
(2E)-N-(4-methylphenyl)-2-(quinolin-2-ylmethylidene)hydrazinecarboxamide	-	Homo sapiens
(2E)-N-benzyl-2-(quinolin-2-ylmethylidene)hydrazinecarbothioamide	-	Homo sapiens
(2E)-N-phenyl-2-(quinolin-2-ylmethylidene)hydrazinecarbothioamide	-	Homo sapiens
(2E)-N-[2',6'-di(propan-2-yl)biphenyl-4-yl]-2-(quinolin-2-ylmethylidene)hydrazinecarbothioamide	-	Homo sapiens
additional information	IC50 values for in vivo inhibition of the enzyme in human cancer cell lines, overview	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	-	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
HeLa cell	-	Homo sapiens	-
HL-60 cell	-	Homo sapiens	-
HT-29 cell	-	Homo sapiens	-
K-562 cell	-	Homo sapiens	-
SGC-7901 cell	-	Homo sapiens	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
additional information	substrate for topo IIalpha is supercoiled pBR322 plasmid DNA. Topo II-mediated DNA strand passage requires ATP binding, so reactions in the absence of ATP represent the cleavage and relegation events that take place prior to topo II catalyzed DNA strand passage	Homo sapiens	?	-	?

Synonyms

Synonyms	Comment	Organism
Topo IIalpha	-	Homo sapiens
topoisomerase IIalpha	-	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
8	-	assay at	Homo sapiens

Cofactor

Cofactor	Comment	Organism	Structure
ATP	-	Homo sapiens

General Information

General Information	Comment	Organism
physiological function	topo IIalpha has essential roles in sister chromatid separation at anaphase	Homo sapiens