Inhibitors | Comment | Organism | Structure |
---|---|---|---|
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 | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P11387 | - |
- |
Synonyms | Comment | Organism |
---|---|---|
Top1 | - |
Homo sapiens |
Topoisomerase I | - |
Homo sapiens |