Literature summary for 5.6.2.1 extracted from

Nagarajan, M.; Morrell, A.; Antony, S.; Kohlhagen, G.; Agama, K.; Pommier, Y.; Ragazzon, P.A.; Garbett, N.C.; Chaires, J.B.; Hollingshead, M.; Cushman, M.
Synthesis and biological evaluation of bisindenoisoquinolines as topoisomerase I inhibitors (2006), J. Med. Chem., 49, 5129-5140.

Inhibitors

Inhibitors	Comment	Organism
1,3-[6-(3-Amino-1-propyl)-5,6-dihydro-2,3-dimethoxy-8,9-methylenedioxy-5,11-dioxo-11H-indeno[1,2-c]isoquinoline]-[5',6'-dihydro-6'-(3'-amino-1'-propyl)-5',11'-dioxo-11'H-indeno[1,2-c]-isoquinoline]propane bis(trifluoroacetate)	-	Homo sapiens
6-(3-aminopropyl)-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione	class of non-camptothecin topoisomerase I inhibitors, exert cytotoxicity by trapping the covalent complex formed between DNA and Top1during relaxation of DNA supercoils	Homo sapiens
bis-1,2-[(5,6-dihydro-5,11-diketo-11H-indeno[1,2-c]isoquinoline)-6-(ethylamino)-ethylamino]ethane tetra(trifluoroacetate)	-	Homo sapiens
bis-1,2-[(5,6-dihydro-5,11-diketo-11H-indeno[1,2-c]isoquinoline)-6-ethylamino]ethane bis(trifluoroacetate)	weak activity	Homo sapiens
bis-1,2-[(5,6-dihydro-5,11-diketo-11H-indeno[1,2-c]isoquinoline)-6-propylamino]ethane bis(trifluoroacetate)	similar activity as 1 microM camptothecin	Homo sapiens
bis-1,3-[(5,6-dihydro-5,11-diketo-11H-indeno[1,2-c]isoquinoline)-6-ethylamino]propane bis(trifluoroacetate)	similar activity as 1 microM camptothecin	Homo sapiens
bis-1,3-[(5,6-dihydro-5,11-diketo-11H-indeno[1,2-c]isoquinoline)-6-propylamino]propane bis(trifluoroacetate)	similar activity as 1 microM camptothecin	Homo sapiens
bis-1,3-[(5,6-dihydro-5,11-diketo-2,3-dimethoxy-11H-indeno-[1,2-c]isoquinoline)-6-ethylamino]propane bis(trifluoroacetate)	-	Homo sapiens
bis-1,3-[(5,6-dihydro-5,11-diketo-2,3-dimethoxy-11H-indeno-[1,2-c]isoquinoline)-6-propylamino]propane bis(trifluoroacetate)	-	Homo sapiens
bis-1,3-[(5,6-dihydro-5,11-diketo-3-nitro-11H-indeno[1,2-c]isoquinoline)-6-ethylamino]propane bis(trifluoroacetate)	-	Homo sapiens
bis-1,4-[(5,6-dihydro-5,11-diketo-11H-indeno[1,2-c]isoquinoline)-(6-propyl-tert-BOCamino)]butane	weak activity	Homo sapiens
bis-1,4-[(5,6-dihydro-5,11-diketo-11H-indeno[1,2-c]isoquinoline)-6-propylamino]butane bis(trifluoroacetate)	similar activity as 6-(3-aminopropyl)-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione	Homo sapiens
bis[(5,6-dihydro-5,11-diketo-11H-indeno[1,2-c]isoquinoline)-6-(ethylamino)-ethyl]amine tris(trifluoroacetate)	similar activity as 6-(3-aminopropyl)-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione	Homo sapiens
bis[(5,6-dihydro-5,11-diketo-11H-indeno[1,2-c]isoquinoline)-6-ethyl]amine	weak activity	Homo sapiens
bis[(5,6-dihydro-5,11-diketo-11H-indeno[1,2-c]isoquinoline)-6-propyl]amine	weak activity	Homo sapiens
bis[(5,6-dihydro-5,11-diketo-11H-indeno[1,2-c]isoquinoline)-6-propyl]methylamine	weak activity	Homo sapiens
bis[(5,6-dihydro-5,11-diketo-11H-indeno[1,2-c]isoquinoline)]-(6-ethyl,6'-propyl)ammonium Trifluoroacetate	weak activity	Homo sapiens
bis[(5,6-dihydro-5,11-diketo-11H-indeno[1,2-c]isoquinoline)]-(6-propyl,6'-butyl)amine hydrochloride	weak activity	Homo sapiens
camptothecin	-	Homo sapiens
additional information	biological results for substituted compounds revealed a disagreement between the structure-activity relationships of monomeric indenoisoquinoline and bisindenoisoquinoline as Top1 inhibitors, but cytotoxicity maintained for both series of compounds. Bisindenoisoquinoline to determine effect of indenoisoquinoline dimerization on cytotoxicity and Top1 inhibition. It is conceivable that it could exert antitumor activity by targeting DNA itself, apart from Top1	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	P11387	-	-

Synonyms

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