Literature summary for 5.6.2.2 extracted from

Oksuzoglu, E.; Tekiner-Gulbas, B.; Alper, S.; Temiz-Arpaci, O.; Ertan, T.; Yildiz, I.; Diril, N.; Sener-Aki, E.; Yalcin, I.
Some benzoxazoles and benzimidazoles as DNA topoisomerase I and II inhibitors (2008), J. Enzyme Inhib. Med. Chem., 23, 37-42.

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Inhibitors

Inhibitors	Comment	Organism	Structure
2-(p-nitrobenzyl)benzoxazole	-	Bos taurus
5-amino-2-(4-fluorophenyl)benzoxazole	-	Bos taurus
5-amino-2-(4-methylbenzyl)benzoxazole	-	Bos taurus
5-amino-2-(p-methylbenzyl)benzoxazole	-	Bos taurus
5-amino-2-phenylbenzoxazole	-	Bos taurus
5-chloro-2-(4-methylphenyl)benzoxazole	-	Bos taurus
5-chloro-2-(p-methylphenyl)benzoxalzole	-	Bos taurus
5-nitro-2-(4-nitrobenzyl)benzoxazole	-	Bos taurus
5-nitro-2-(p-nitrobenzyl)benzoxazole	-	Bos taurus
5-nitro-2-phenoxymethyl-benzimidazole	-	Bos taurus
etoposide	-	Bos taurus
additional information	not inhibited by camptothecin, 2-phenoxymethylbenzimidazole, 5-amino-2-(p-bromophenyl)benzoxazole, and 2-(p-chlorobenzyl)benzoxazole	Bos taurus

Organism

Organism	UniProt	Comment	Textmining
Bos taurus	-	-	-
Bos taurus	Q7M3G2	fragments	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
thymus	-	Bos taurus	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
supercoiled DNA + ATP + H2O	-	Bos taurus	catenated DNA networks + ADP + phosphate	-	?

Synonyms

Synonyms	Comment	Organism
DNA topoisomerase II	-	Bos taurus

Cofactor

Cofactor	Comment	Organism	Structure
ATP	-	Bos taurus

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.0174	-	-	Bos taurus	2-(p-nitrobenzyl)benzoxazole
0.0223	-	-	Bos taurus	5-chloro-2-(4-methylphenyl)benzoxazole
0.09141	-	-	Bos taurus	5-nitro-2-(4-nitrobenzyl)benzoxazole
0.17	-	-	Bos taurus	etoposide
0.1867	-	-	Bos taurus	5-amino-4-(p-methylbenzyl)benzoxazole
0.4878	-	-	Bos taurus	5-amino-4-(p-fluorophenyl)benzoxazole
0.58	-	-	Bos taurus	5-amino-4-phenylbenzoxazole

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Release 2023.1 (January 2023)