Application | Comment | Organism |
---|---|---|
drug development | Top1 inhibitors approved for the treatment of cancer | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
2,3-dimethoxy-6-methyl-5H-[1,3]dioxolo[5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione | novel functionalities appended to the lactam side chain of the indenoisoquinolines. Development of indenoisoquinoline Top1 inhibitors where the di(methoxy) and methylenedioxy substituents on the aromatic nucleus are combined with previously utilized and novel heterocyclic lactam side chains in an effort to improve the anticancer activity of the indenoisoquinolines | Homo sapiens | |
3-(2,3-dimethoxy-5,12-dioxo-5,12-dihydro-6H-[1,3]dioxolo[5,6]indeno[1,2-c]isoquinolin-6-yl)propan-1-aminium chloride | higher activity than the parent compound 2,3-dimethoxy-6-methyl-5H-[1,3]dioxolo[5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione | Homo sapiens | |
3-(imidazolyl-1-propyl)-5,6-dihydro-2,3-dimethoxy-8,9-methylenedioxy-5,11-dioxo-11H-indeno[1,2-c]isoquinoline hydrochloride | higher activity than the parent compound 2,3-dimethoxy-6-methyl-5H-[1,3]dioxolo[5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione | Homo sapiens | |
3-[(1-hydroxyethyl-piperazine)-1-propyl]-5,6-dihydro-2,3-dimethoxy-8,9-methylenedioxy-5,11-dioxo-11H-indeno[1,2-c]isoquinoline | similar activity as the parent compound 2,3-dimethoxy-6-methyl-5H-[1,3]dioxolo[5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione | Homo sapiens | |
3-[(1-methylpiperazinyl)-1-propyl]-5,6-dihydro-2,3-dimethoxy-8,9-methylenedioxy-5,11-dioxo-11H-indeno[1,2-c]isoquinoline | weak activity | Homo sapiens | |
3-[(morpholinyl)-1-propyl]-5,6-dihydro-2,3-dimethoxy-8,9-methylenedioxy-5,11-dioxo-11H-indeno[1,2-c]isoquinoline | higher activity than the parent compound 2,3-dimethoxy-6-methyl-5H-[1,3]dioxolo[5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione | Homo sapiens | |
3-[(thiomorpholinyl)-1-propyl]-5,6-dihydro-2,3-dimethoxy-8,9-methylenedioxy-5,11-dioxo-11H-indeno[1,2-c]isoquinoline | similar activity as the parent compound 2,3-dimethoxy-6-methyl-5H-[1,3]dioxolo[5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione | Homo sapiens | |
6-(3-homopiperazinyl-1-propyl)-5,6-dihydro-2,3-dimethoxy-8,9-methylenedioxy-5,11-dioxo-11H-indeno[1,2-c]isoquinoline dihydrochloride | higher activity than the parent compound 2,3-dimethoxy-6-methyl-5H-[1,3]dioxolo[5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione | Homo sapiens | |
6-(3-piperazinyl-1-propyl)-5,6-dihydro-2,3-dimethoxy-8,9-methylenedioxy-5,11-dioxo-11H-indeno[1,2-c]isoquinoline dihydrochloride | similar activity as the parent compound 2,3-dimethoxy-6-methyl-5H-[1,3]dioxolo[5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione | Homo sapiens | |
6-(3-thiazolylamino-1-propyl)-5,6-dihydro-2,3-dimethoxy-8,9-methylenedioxy-5,11-dioxo-11H-indeno[1,2-c]isoquinoline dihydrochloride | higher activity than the parent compound 2,3-dimethoxy-6-methyl-5H-[1,3]dioxolo[5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione | Homo sapiens | |
6-[(3-morpholylethylamino)-1-propyl]-5,6-dihydro-2,3-dimethoxy-8,9-methylenedioxy-5,11-dioxo-11H-indeno[1,2-c]isoquinoline | higher activity than the parent compound 2,3-dimethoxy-6-methyl-5H-[1,3]dioxolo[5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione | Homo sapiens | |
6-[3-(1H-imidazol-1-yl)propyl]-2,3-dimethoxy-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione | higher activity than the parent compound 2,3-dimethoxy-6-methyl-5H-[1,3]dioxolo[5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione | Homo sapiens | |
6-[3-(1H-imidazol-1-yl)propyl]-3-nitro-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione hydrochloride | higher activity than the parent compound 2,3-dimethoxy-6-methyl-5H-[1,3]dioxolo[5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione | Homo sapiens | |
6-[3-(1H-imidazol-1-yl)propyl]-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione | higher activity than the parent compound 2,3-dimethoxy-6-methyl-5H-[1,3]dioxolo[5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione | Homo sapiens | |
6-[3-(3-hydroxypiperidinyl)-1-propyl]-5,6-dihydro-2,3-dimethoxy-8,9-methylenedioxy-5,11-dioxo-11H-indeno[1,2-c]isoquinoline hydrochloride | higher activity than the parent compound 2,3-dimethoxy-6-methyl-5H-[1,3]dioxolo[5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione | Homo sapiens | |
6-[3-(4-aminopiperidinyl)-1-propyl]-5,6-dihydro-2,3-dimethoxy-8,9-methylenedioxy-5,11-dioxo-11H-indeno[1,2-c]isoquinoline dihydrochloride | weak activity | Homo sapiens | |
6-[3-pyrazolyl-1-propyl]-5,6-dihydro-2,3-dimethoxy-8,9-methylenedioxy-5,11-dioxo-11H-indeno[1,2-c]isoquinoline | similar activity as the parent compound 2,3-dimethoxy-6-methyl-5H-[1,3]dioxolo[5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione | Homo sapiens | |
6-[3-[2-(1,2,4)]-triazolyl-1-propyl]-5,6-dihydro-2,3-dimethoxy-8,9-methylenedioxy-5,11-dioxo-11H-indeno[1,2-c]isoquinoline hydrochloride | higher activity than the parent compound 2,3-dimethoxy-6-methyl-5H-[1,3]dioxolo[5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione | Homo sapiens | |
camptothecin | - |
Homo sapiens | |
additional information | indenoisoquinoline topoisomerase I (Top1) inhibitors. lactam substituents possessing nitrogen heterocycles can provide highly cytotoxic compounds with potent Top1 inhibition. Molecular modeling of these compounds in complex with DNA and Top1 suggests that some of the lactam substituents are capable of interacting with the DNA base pairs above and below the site of intercalation and/or with Top1 amino acid residues, resulting in increased biological activity | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Synonyms | Comment | Organism |
---|---|---|
Top1 | - |
Homo sapiens |
Topoisomerase I | - |
Homo sapiens |