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 | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
nucleus | - |
Homo sapiens | 5634 | - |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Mg2+ | - |
Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
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 | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | substrate is pBR322 DNA, structure-activity relationship study, overview | Homo sapiens | ? | - |
? |
Subunits | Comment | Organism |
---|---|---|
More | structure-activity relationship study, overview | Homo sapiens |
Synonyms | Comment | Organism |
---|---|---|
Topoisomerase I | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
30 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.9 | - |
assay at | Homo sapiens |
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 |