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Literature summary for 5.6.2.1 extracted from

  • Thapa, P.; Karki, R.; Thapa, U.; Jahng, Y.; Jung, M.J.; Nam, J.M.; Na, Y.; Kwon, Y.; Lee, E.S.
    2-Thienyl-4-furyl-6-aryl pyridine derivatives: synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship study (2010), Bioorg. Med. Chem., 18, 377-386.
    View publication on PubMed
Search for more literature for 5.6.2.1

Inhibitors

Inhibitors Comment Organism Structure
2-(4-chlorophenyl)-4-(furan-3-yl)-6-(3-methylthiophen-2-yl) pyridine 86% inhibition at 0.1 mM Homo sapiens
2-(4-chlorophenyl)-6-(5-chlorothiophen-2-yl)-4-(furan-2-yl) pyridine 53% inhibition at 0.1 mM Homo sapiens
2-(5-chlorothiophen-2-yl)-4-(furan-3-yl)-6-(5-methylfuran-2-yl) pyridine 13.2% inhibition at 0.1 mM Homo sapiens
2-(5-chlorothiophen-2-yl)-4-(furan-3-yl)-6-o-tolylpyridine 4.6% inhibition at 0.1 mM Homo sapiens
2-(5-chlorothiophen-2-yl)-6-(furan-2-yl)-4-(furan-3-yl)pyridine 9.6% inhibition at 0.1 mM Homo sapiens
2-(furan-2-yl)-4-(furan-3-yl)-6-(3-methylthiophen-2-yl)pyridine 5.4% inhibition at 0.1 mM Homo sapiens
4-(5-chlorofuran-2-yl)-2-(3-chlorophenyl)-6-(3-methylthiophen-2-yl) pyridine 5.9% inhibition at 0.1 mM Homo sapiens
4-(5-chlorofuran-2-yl)-2-(3-chlorophenyl)-6-(5-chlorothiophen-2-yl) pyridine 13% inhibition at 0.1 mM Homo sapiens
4-(5-chlorofuran-2-yl)-2-(4-chlorophenyl)-6-(3-methylthiophen-2-yl) pyridine 5.1% inhibition at 0.1 mM Homo sapiens
4-(5-chlorofuran-2-yl)-2-(5-chlorothiophen-2-yl)-6-(furan-2-yl) pyridine 23% inhibition at 0.1 mM Homo sapiens
4-(5-chlorofuran-2-yl)-2-(5-chlorothiophen-2-yl)-6-p-tolylpyridine 14% inhibition at 0.1 mM Homo sapiens
4-(5-chlorofuran-2-yl)-2-(furan-2-yl)-6-(3-methylthiophen-2-yl) pyridine 7.8% inhibition at 0.1 mM Homo sapiens
4-(5-chlorofuran-2-yl)-6-(3-methylthiophen-2-yl)-2,3'-bipyridine 21% inhibition at 0.1 mM Homo sapiens
camptothecin 79% inhibition at 0.1 mM Homo sapiens
additional information design and synthesis of 60 2-thienyl-4-furyl-6-aryl pyridine derivatives, inhibitory potency and cytotoxicity analysis using human topoisomerase I and human cancer cell lines MCF-7, HeLa, DU145, and K562. The 2-(5-chlorothiophen-2-yl)-4-(furan-3-yl) moiety has an important role in displaying biological activities. No or poor inhibition by 2-(2-chlorophenyl)-4-(furan-2-yl)-6-(3-methylthiophen-2-yl) pyridine, 2-(4-chlorophenyl)-4-(furan-2-yl)-6-(3-methylthiophen-2-yl) pyridine, 2-(5-chlorothiophen-2-yl)-4-(furan-3-yl)-6-m-tolylpyridine, 2-(5-chlorothiophen-2-yl)-4-(furan-3-yl)-6-p-tolylpyridine, 2-(2-chlorophenyl)-6-(5-chlorothiophen-2-yl)-4-(furan-3-yl) pyridine, 2-(3-chlorophenyl)-6-(5-chlorothiophen-2-yl)-4-(furan-3-yl) pyridine, 2-(4-chlorophenyl)-6-(5-chlorothiophen-2-yl)-4-(furan-3-yl) pyridine, 6-(5-chlorothiophen-2-yl)-4-(furan-3-yl)-2, 2'-bipyridine, 6-(5-chlorothiophen-2-yl)-4-(furan-3-yl)-2,30-bipyridine, and 4-(5-chlorofuran-2-yl)-2-(4-chlorophenyl)-6-(5-chlorothiophen-2-yl) pyridine Homo sapiens

Localization

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

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
carcinoma cell
-
 Homo sapiens
-
DU-145 cell
-
 Homo sapiens
-
HCT-15 cell
-
 Homo sapiens
-
HeLa cell
-
 Homo sapiens
-
K-562 cell
-
 Homo sapiens
-
MCF-7 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information substrate is pBR322 DNA, structure-activity relationship study, overview Homo sapiens ?
-
 ?

Subunits

Subunits Comment Organism
More structure-activity relationship study, overview Homo sapiens

Synonyms

Synonyms Comment Organism
Topoisomerase I
-
 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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
additional information
-
 2-thienyl-4-furyl-6-aryl pyridine derivatives, IC50 values in cytotoxicity assays in cancer cell lines, overview Homo sapiens additional information