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Literature summary for 5.6.2.2 extracted from

  • Thapa, U.; Thapa, P.; Karki, R.; Yun, M.; Choi, J.H.; Jahng, Y.; Lee, E.; Jeon, K.H.; Na, Y.; Ha, E.M.; Cho, W.J.; Kwon, Y.; Lee, E.S.
    Synthesis of 2,4-diaryl chromenopyridines and evaluation of their topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship (2011), Eur. J. Med. Chem., 46, 3201-3209.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
2,4-di(furan-2-yl)-5H-chromeno[4,3-b]pyridine 11.6% inhibition at 0.1 mM Homo sapiens
2,4-di(pyridin-2-yl)-5H-chromeno[4,3-b]pyridine 10.6% inhibition at 0.1 mM Homo sapiens
2,4-di(thiophen-2-yl)-5H-chromeno[4,3-b]pyridine 7.9% inhibition at 0.1 mM Homo sapiens
2,4-di(thiophen-3-yl)-5H-chromeno[4,3-b]pyridine
-
Homo sapiens
2,4-diphenyl-5H-chromeno[4,3-b]pyridine 15.4% inhibition at 0.1 mM Homo sapiens
2-(furan-2-yl)-4-(pyridin-2-yl)-5H-chromeno[4,3-b]pyridine 2.0% inhibition at 0.1 mM Homo sapiens
2-(furan-2-yl)-4-(pyridin-3-yl)-5H-chromeno[4,3-b]pyridine 5.6% inhibition at 0.1 mM Homo sapiens
2-(furan-2-yl)-4-(thiophen-2-yl)-5H-chromeno[4,3-b]pyridine 6.8% inhibition at 0.1 mM Homo sapiens
2-(furan-2-yl)-4-phenyl-5H-chromeno[4,3-b]pyridine 28.4% inhibition at 0.1 mM Homo sapiens
2-(pyridin-2-yl)-4-(pyridin-3-yl)-5H-chromeno[4,3-b]pyridine 8.6% inhibition at 0.1 mM Homo sapiens
2-(pyridin-2-yl)-4-(thiophen-2-yl)-5H-chromeno[4,3-b]pyridine 19.4% inhibition at 0.1 mM Homo sapiens
2-phenyl-4-(pyridin-2-yl)-5H-chromeno[4,3-b]pyridine 8.6% inhibition at 0.1 mM Homo sapiens
2-phenyl-4-(pyridin-3-yl)-5H-chromeno[4,3-b]pyridine 14.0% inhibition at 0.1 mM Homo sapiens
2-phenyl-4-(thiophen-2-yl)-5H-chromeno[4,3-b]pyridine 10.8% inhibition at 0.1 mM Homo sapiens
2-phenyl-4-(thiophen-3-yl)-5H-chromeno[4,3-b]pyridine 17.6% inhibition at 0.1 mM Homo sapiens
4-(furan-2-yl)-2-(pyridin-2-yl)-5H-chromeno[4,3-b]pyridine 23.4% inhibition at 0.1 mM Homo sapiens
4-(furan-2-yl)-2-(thiophen-2-yl)-5H-chromeno [4,3-b]pyridine 14.1% inhibition at 0.1 mM Homo sapiens
4-(furan-2-yl)-2-(thiophen-2-yl)-5H-chromeno[4,3-b]pyridine
-
Homo sapiens
4-(furan-2-yl)-2-phenyl-5H-chromeno[4,3-b]pyridine 11.5% inhibition at 0.1 mM Homo sapiens
4-(furan-3-yl)-2-(thiophen-2-yl)-5H-chromeno[4,3-b]pyridine 8.4% inhibition at 0.1 mM Homo sapiens
4-(furan-3-yl)-2-phenyl-5H-chromeno[4,3-b]pyridine 10.5% inhibition at 0.1 mM Homo sapiens
4-(pyridin-2-yl)-2-(thiophen-2-yl)-5H-chromeno[4,3-b]pyridine 8.5% inhibition at 0.1 mM Homo sapiens
4-(pyridin-2-yl)-2-(thiophen-3-yl)-5H-chromeno[4,3-b]pyridine 25.3% inhibition at 0.1 mM Homo sapiens
4-phenyl-2-(pyridin-2-yl)-5H-chromeno[4,3-b]pyridine 7.2% inhibition at 0.1 mM Homo sapiens
4-phenyl-2-(thiophen-2-yl)-5H-chromeno[4,3-b]pyridine 7.5% inhibition at 0.1 mM Homo sapiens
camptothecin
-
Homo sapiens
etoposide
-
Homo sapiens
additional information synthesis of 2,4-diaryl chromenopyridines and evaluation of their topoisomerase II inhibitory activity, cytotoxicity, and structure-activity relationship, overview. 2-Furyl or 2-thienyl at 2- or 4-position of central pyridine is crucial in displaying topo I or II inhibitory activity and cytotoxicity Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
nucleus
-
Homo sapiens 5634
-

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ required Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
commercial preparation DNA topo IIalpha Homo sapiens
-
DU-145 cell a prostate tumor cell line Homo sapiens
-
HCT-15 cell a colorectal adenocarcinoma cell line Homo sapiens
-
HeLa cell
-
Homo sapiens
-
HL-60 cell a myeloid leukemic tumor cell line Homo sapiens
-
MDA-MB-231 cell a breast tumor cell line Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information substrate for DNA topo IIalpha is supercoiled pBR322 plasmid DNA Homo sapiens ?
-
?

Synonyms

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

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
30
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.9
-
assay at Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
Homo sapiens