Literature summary for 5.6.2.1 extracted from

Cinelli, M.A.; Cordero, B.; Dexheimer, T.S.; Pommier, Y.; Cushman, M.
Synthesis and biological evaluation of 14-(aminoalkyl-aminomethyl)aromathecins as topoisomerase I inhibitors: investigating the hypothesis of shared structure-activity relationships (2009), Bioorg. Med. Chem., 17, 7145-7155.

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Inhibitors

Inhibitors	Comment	Organism	Structure
12H-5,11a-diazadibenzo[b,h]fluoren-11-one	i.e. rosettacin	Homo sapiens
14-(10'-aminodecyl-1'-aminomethyl)-12H-5,11a-diazadibenzo[b,h]fluoren-11-one trihydrochloride	-	Homo sapiens
14-(11'-aminoundecyl-1'-aminomethyl)-12H-5,11a-diazadibenzo[b,h]fluoren-11-one trihydrochloride	-	Homo sapiens
14-(12'-aminododecyl-1'-aminomethyl)-12H-5,11a-diazadibenzo[b,h]fluoren-11-one trihydrochloride	-	Homo sapiens
14-(2'-aminoethyl-1'-aminomethyl)-12H-5,11a-diazadibenzo[b,h]fluoren-11-one trihydrochloride	-	Homo sapiens
14-(3'-aminopropyl-1'-aminomethyl)-12H-5,11a-diazadibenzo[b,h]fluoren-11-one trihydrochloride	-	Homo sapiens
14-(4'-aminobutyl-1'-aminomethyl)-12H-5,11a-diazadibenzo[b,h]fluoren-11-one trihydrochloride	-	Homo sapiens
14-(5'-aminopentyl-1'-aminomethyl)-12H-5,11a-diazadibenzo[b,h]fluoren-11-one trihydrochloride	-	Homo sapiens
14-(6'-aminohexyl-1'-aminomethyl)-12H-5,11a-diazadibenzo[b,h]fluoren-11-one trihydrochloride	-	Homo sapiens
14-(7'-aminoheptyl-1'-aminomethyl)-12H-5,11a-diazadibenzo[b,h]fluoren-11-one trihydrochloride	-	Homo sapiens
14-(8'-aminooctyl-1'-aminomethyl)-12H-5,11a-diazadibenzo[b,h]fluoren-11-one trihydrochloride	-	Homo sapiens
14-(9'-aminononyl-1'-aminomethyl)-12H-5,11a-diazadibenzo[b,h]fluoren-11-one trihydrochloride	-	Homo sapiens
2,3-dimethoxy-6-methyl-5H-[1,3]dioxolo[5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione	i.e. NSC314622	Homo sapiens
6-{3-[(2-hydroxyethyl)amino]propyl}-2,3-dimethoxy-5H-[1,3]dioxolo[5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione	i.e. MJ-III-65	Homo sapiens
camptothecin	-	Homo sapiens
indenoisoquinoline	-	Homo sapiens
irinotecan	-	Homo sapiens
additional information	synthesis and inhibitory potency of a series of water-soluble aromathecins substituted at position 14 with diaminoalkanes of various lengths, that all show antiproliferative potency. Aromathecins with longer diaminoalkane substituents over 6Cs possess lower anti-top1 activity than their smaller counterparts with 2-4 Cs	Homo sapiens
topotecan	-	Homo sapiens

Metals/Ions

Metals/Ions	Comment	Organism	Structure
Mg2+	-	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	P11387	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
additional information	recombinant enzyme	Homo sapiens	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
additional information	structure-activity relationship, overview	Homo sapiens	?	-	?

Subunits

Subunits	Comment	Organism
More	structure-activity relationship, overview	Homo sapiens

Synonyms

Synonyms	Comment	Organism
Top1	-	Homo sapiens
Topoisomerase I	-	Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C]	Temperature Optimum Maximum [°C]	Comment	Organism
25	-	assay at	Homo sapiens

pH Optimum

pH Optimum Minimum	pH Optimum Maximum	Comment	Organism
7.5	-	assay at	Homo sapiens

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Release 2023.1 (January 2023)