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Literature summary for 5.6.2.1 extracted from

  • Basnet, A.; Thapa, P.; Karki, R.; Na, Y.; Jahng, Y.; Jeong, B.S.; Jeong, T.C.; Lee, C.S.; Lee, E.S.
    2,4,6-Trisubstituted pyridines: Synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship (2007), Bioorg. Med. Chem., 15, 4351-4359.
    View publication on PubMed

Application

Application Comment Organism
pharmacology Topo I targets for design of antitumor agents Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
4-(furan-3-yl)-6-(thiophene-2-yl)-[2,4']-bipyridyl shows moderate topoisomerase I inhibitory activities when compared to camptothecin Homo sapiens
4-(furan-3-yl)-6-(thiophene-3-yl)-[2,4']-bipyridyl shows moderate topoisomerase I inhibitory activities when compared to camptothecin Homo sapiens
4-(thiophene-3-yl)-6-(thiophene-2-yl)-[2,2']-bipyridyl shows significant topoisomerase I inhibitory activities at 20 microM and 100 microM concentration Homo sapiens
4-(thiophene-3-yl)-6-(thiophene-2-yl)-[2,4']-bipyridyl shows significant topoisomerase I inhibitory activities at 20 microM and 100 microM concentration Homo sapiens
6'-(thiophene-2-yl)-[3,4',2',4'']-terpyridine shows moderate topoisomerase I inhibitory activities when compared to camptothecin Homo sapiens
6'-(thiophene-2-yl)-[4,2',4',4'']-terpyridine shows moderate topoisomerase I inhibitory activities when compared to camptothecin Homo sapiens
6-(furan-2-yl)-4-(furan-3-yl)-[2,2']-bipyridyl shows moderate topoisomerase I inhibitory activities when compared to camptothecin Homo sapiens
6-(furan-2-yl)-4-(furan-3-yl)-[2,4']-bipyridyl shows moderate topoisomerase I inhibitory activities when compared to camptothecin Homo sapiens
6-(furan-2-yl)-4-(thiophene-2-yl)-[2,4']-bipyridyl shows significant topoisomerase I inhibitory activities at 20 microM and 100 microM concentration Homo sapiens
6-(furan-2-yl)-4-(thiophene-3-yl)-[2,4']-bipyridyl shows moderate topoisomerase I inhibitory activities when compared to camptothecin Homo sapiens
6-(furan-2-yl)-[3,4',2',4'']-terpyridine shows significant topoisomerase I inhibitory activities at 20 microM and 100 microM concentration Homo sapiens
camptothecin Topoisomerase I inhibitor added for measuring the inhibition of DNA relaxation Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Synonyms

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