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Literature summary for 5.6.2.2 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 II have been attractive targets for design of antitumor agents Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
4-(furan-3-yl)-6-(thiophene-2-yl)-[2,4']-bipyridyl significant inhibitory effects on human DNA Topo II at 20 microM and 100 microM concentration Homo sapiens
4-(furan-3-yl)-6-(thiophene-3-yl)-[2,4']-bipyridyl significant inhibitory effects on human DNA Topo II at 20 microM and 100 microM concentration Homo sapiens
4-(thiophene-3-yl)-6-(thiophene-2-yl)-[2,2']-bipyridyl weak inhibitory effects on human DNA Topo II compared to etoposide Homo sapiens
4-(thiophene-3-yl)-6-(thiophene-2-yl)-[2,4']-bipyridyl weak inhibitory effects on human DNA Topo II when compared to etoposide Homo sapiens
6'-(thiophene-2-yl)-[3,4',2',4'']-terpyridine significant inhibitory effects on human DNA Topo II at 20 microM and 100 microM concentration Homo sapiens
6'-(thiophene-2-yl)-[4,2',4',4'']-terpyridine significant inhibitory effects on human DNA Topo II at 20 microM and 100 microM concentration Homo sapiens
6-(furan-2-yl)-4-(furan-3-yl)-[2,2']-bipyridyl significant inhibitory effects on human DNA Topo II at 20 microM and 100 microM concentration Homo sapiens
6-(furan-2-yl)-4-(furan-3-yl)-[2,4']-bipyridyl significant inhibitory effects on human DNA Topo II at 20 microM and 100 microM concentration Homo sapiens
6-(furan-2-yl)-4-(thiophene-2-yl)-[2,4']-bipyridyl weak inhibitory effects on human DNA Topo II compared to etoposide Homo sapiens
6-(furan-2-yl)-4-(thiophene-3-yl)-[2,4']-bipyridyl significant inhibitory effects on human DNA Topo II at 20 microM and 100 microM concentration Homo sapiens
6-(furan-2-yl)-[3,4',2',4'']-terpyridine weak inhibitory effects on human DNA Topo II compared to etoposide Homo sapiens
etoposide Topoisomerase II inhibitor added for measuring the inhibition of DNA relaxation Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Synonyms

Synonyms Comment Organism
DNA Topo II
-
Homo sapiens
topo II
-
Homo sapiens
Topoisomerase II
-
Homo sapiens