Synthesis and characterization of pyrazoleanthrone derivatives as Aurora A kinase inhibitors
Abstract Aurora A is a cell cycle kinase linked to cancer. For the purpose of finding biologically active of novel compounds and providing new ideas for drug-design, we performed virtual screening in commercially available databases and got pyrazoleanthrone with promising inhibitory activity against...
Ausführliche Beschreibung
Gespeichert in:
| Autor*in: |
Sun, Xiao-xiao [verfasserIn] Sun, Tao [verfasserIn] Wang, Tai-yi [verfasserIn] Zhang, Yan [verfasserIn] Liu, Hui-juan [verfasserIn] Wang, Quan [verfasserIn] Niu, Guo-jun [verfasserIn] Liu, Wei [verfasserIn] Zhou, Hong-gang [verfasserIn] Yang, Cheng [verfasserIn] |
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| Format: |
E-Artikel |
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| Sprache: |
Englisch |
| Erschienen: |
2013 |
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| Schlagwörter: |
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| Übergeordnetes Werk: |
Enthalten in: Chemical Research in Chinese Universities - Jilin University and The Editorial Department of Chemical Research in Chinese Universities, 2012, 29(2013), 6 vom: 29. Okt., Seite 1098-1103 |
|---|---|
| Übergeordnetes Werk: |
volume:29 ; year:2013 ; number:6 ; day:29 ; month:10 ; pages:1098-1103 |
| Links: |
|---|
| DOI / URN: |
10.1007/s40242-013-3216-2 |
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SPR032910231 |
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| 520 | |a Abstract Aurora A is a cell cycle kinase linked to cancer. For the purpose of finding biologically active of novel compounds and providing new ideas for drug-design, we performed virtual screening in commercially available databases and got pyrazoleanthrone with promising inhibitory activity against Aurora A. Optimization of solvent accessible C7 position of pyrazoleanthrone made us get thirteen target compounds. These pyrazoleanthrone derivatives were evaluated by Aurora A inhibition assays in vitro. The results show that some target compounds could inhibit Aurora A kinase. Meanwhile, these title compounds were tested in vitro against hepatocellular carcinoma(HepG2) cells by the 3′-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide(MTT) method, showing that most of them had inhibitory potency. The inhibition rate of compound 6h was about 80% against HepG2 cells, and the $ IC_{50} $ value was 17.4 μmol/L, which would be considered for further study. | ||
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| 700 | 1 | |a Wang, Quan |e verfasserin |4 aut | |
| 700 | 1 | |a Niu, Guo-jun |e verfasserin |4 aut | |
| 700 | 1 | |a Liu, Wei |e verfasserin |4 aut | |
| 700 | 1 | |a Zhou, Hong-gang |e verfasserin |4 aut | |
| 700 | 1 | |a Yang, Cheng |e verfasserin |4 aut | |
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10.1007/s40242-013-3216-2 doi (DE-627)SPR032910231 (SPR)s40242-013-3216-2-e DE-627 ger DE-627 rakwb eng Sun, Xiao-xiao verfasserin aut Synthesis and characterization of pyrazoleanthrone derivatives as Aurora A kinase inhibitors 2013 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Abstract Aurora A is a cell cycle kinase linked to cancer. For the purpose of finding biologically active of novel compounds and providing new ideas for drug-design, we performed virtual screening in commercially available databases and got pyrazoleanthrone with promising inhibitory activity against Aurora A. Optimization of solvent accessible C7 position of pyrazoleanthrone made us get thirteen target compounds. These pyrazoleanthrone derivatives were evaluated by Aurora A inhibition assays in vitro. The results show that some target compounds could inhibit Aurora A kinase. Meanwhile, these title compounds were tested in vitro against hepatocellular carcinoma(HepG2) cells by the 3′-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide(MTT) method, showing that most of them had inhibitory potency. The inhibition rate of compound 6h was about 80% against HepG2 cells, and the $ IC_{50} $ value was 17.4 μmol/L, which would be considered for further study. Pyrazoleanthrone (dpeaa)DE-He213 Aurora-A kinase (dpeaa)DE-He213 Inhibitor (dpeaa)DE-He213 Biological activity (dpeaa)DE-He213 Sun, Tao verfasserin aut Wang, Tai-yi verfasserin aut Zhang, Yan verfasserin aut Liu, Hui-juan verfasserin aut Wang, Quan verfasserin aut Niu, Guo-jun verfasserin aut Liu, Wei verfasserin aut Zhou, Hong-gang verfasserin aut Yang, Cheng verfasserin aut Enthalten in Chemical Research in Chinese Universities Jilin University and The Editorial Department of Chemical Research in Chinese Universities, 2012 29(2013), 6 vom: 29. Okt., Seite 1098-1103 (DE-627)SPR03290777X nnns volume:29 year:2013 number:6 day:29 month:10 pages:1098-1103 https://dx.doi.org/10.1007/s40242-013-3216-2 lizenzpflichtig Volltext GBV_USEFLAG_A SYSFLAG_A GBV_SPRINGER SSG-OLC-PHA AR 29 2013 6 29 10 1098-1103 |
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10.1007/s40242-013-3216-2 doi (DE-627)SPR032910231 (SPR)s40242-013-3216-2-e DE-627 ger DE-627 rakwb eng Sun, Xiao-xiao verfasserin aut Synthesis and characterization of pyrazoleanthrone derivatives as Aurora A kinase inhibitors 2013 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Abstract Aurora A is a cell cycle kinase linked to cancer. For the purpose of finding biologically active of novel compounds and providing new ideas for drug-design, we performed virtual screening in commercially available databases and got pyrazoleanthrone with promising inhibitory activity against Aurora A. Optimization of solvent accessible C7 position of pyrazoleanthrone made us get thirteen target compounds. These pyrazoleanthrone derivatives were evaluated by Aurora A inhibition assays in vitro. The results show that some target compounds could inhibit Aurora A kinase. Meanwhile, these title compounds were tested in vitro against hepatocellular carcinoma(HepG2) cells by the 3′-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide(MTT) method, showing that most of them had inhibitory potency. The inhibition rate of compound 6h was about 80% against HepG2 cells, and the $ IC_{50} $ value was 17.4 μmol/L, which would be considered for further study. Pyrazoleanthrone (dpeaa)DE-He213 Aurora-A kinase (dpeaa)DE-He213 Inhibitor (dpeaa)DE-He213 Biological activity (dpeaa)DE-He213 Sun, Tao verfasserin aut Wang, Tai-yi verfasserin aut Zhang, Yan verfasserin aut Liu, Hui-juan verfasserin aut Wang, Quan verfasserin aut Niu, Guo-jun verfasserin aut Liu, Wei verfasserin aut Zhou, Hong-gang verfasserin aut Yang, Cheng verfasserin aut Enthalten in Chemical Research in Chinese Universities Jilin University and The Editorial Department of Chemical Research in Chinese Universities, 2012 29(2013), 6 vom: 29. Okt., Seite 1098-1103 (DE-627)SPR03290777X nnns volume:29 year:2013 number:6 day:29 month:10 pages:1098-1103 https://dx.doi.org/10.1007/s40242-013-3216-2 lizenzpflichtig Volltext GBV_USEFLAG_A SYSFLAG_A GBV_SPRINGER SSG-OLC-PHA AR 29 2013 6 29 10 1098-1103 |
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10.1007/s40242-013-3216-2 doi (DE-627)SPR032910231 (SPR)s40242-013-3216-2-e DE-627 ger DE-627 rakwb eng Sun, Xiao-xiao verfasserin aut Synthesis and characterization of pyrazoleanthrone derivatives as Aurora A kinase inhibitors 2013 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Abstract Aurora A is a cell cycle kinase linked to cancer. For the purpose of finding biologically active of novel compounds and providing new ideas for drug-design, we performed virtual screening in commercially available databases and got pyrazoleanthrone with promising inhibitory activity against Aurora A. Optimization of solvent accessible C7 position of pyrazoleanthrone made us get thirteen target compounds. These pyrazoleanthrone derivatives were evaluated by Aurora A inhibition assays in vitro. The results show that some target compounds could inhibit Aurora A kinase. Meanwhile, these title compounds were tested in vitro against hepatocellular carcinoma(HepG2) cells by the 3′-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide(MTT) method, showing that most of them had inhibitory potency. The inhibition rate of compound 6h was about 80% against HepG2 cells, and the $ IC_{50} $ value was 17.4 μmol/L, which would be considered for further study. Pyrazoleanthrone (dpeaa)DE-He213 Aurora-A kinase (dpeaa)DE-He213 Inhibitor (dpeaa)DE-He213 Biological activity (dpeaa)DE-He213 Sun, Tao verfasserin aut Wang, Tai-yi verfasserin aut Zhang, Yan verfasserin aut Liu, Hui-juan verfasserin aut Wang, Quan verfasserin aut Niu, Guo-jun verfasserin aut Liu, Wei verfasserin aut Zhou, Hong-gang verfasserin aut Yang, Cheng verfasserin aut Enthalten in Chemical Research in Chinese Universities Jilin University and The Editorial Department of Chemical Research in Chinese Universities, 2012 29(2013), 6 vom: 29. Okt., Seite 1098-1103 (DE-627)SPR03290777X nnns volume:29 year:2013 number:6 day:29 month:10 pages:1098-1103 https://dx.doi.org/10.1007/s40242-013-3216-2 lizenzpflichtig Volltext GBV_USEFLAG_A SYSFLAG_A GBV_SPRINGER SSG-OLC-PHA AR 29 2013 6 29 10 1098-1103 |
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10.1007/s40242-013-3216-2 doi (DE-627)SPR032910231 (SPR)s40242-013-3216-2-e DE-627 ger DE-627 rakwb eng Sun, Xiao-xiao verfasserin aut Synthesis and characterization of pyrazoleanthrone derivatives as Aurora A kinase inhibitors 2013 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Abstract Aurora A is a cell cycle kinase linked to cancer. For the purpose of finding biologically active of novel compounds and providing new ideas for drug-design, we performed virtual screening in commercially available databases and got pyrazoleanthrone with promising inhibitory activity against Aurora A. Optimization of solvent accessible C7 position of pyrazoleanthrone made us get thirteen target compounds. These pyrazoleanthrone derivatives were evaluated by Aurora A inhibition assays in vitro. The results show that some target compounds could inhibit Aurora A kinase. Meanwhile, these title compounds were tested in vitro against hepatocellular carcinoma(HepG2) cells by the 3′-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide(MTT) method, showing that most of them had inhibitory potency. The inhibition rate of compound 6h was about 80% against HepG2 cells, and the $ IC_{50} $ value was 17.4 μmol/L, which would be considered for further study. Pyrazoleanthrone (dpeaa)DE-He213 Aurora-A kinase (dpeaa)DE-He213 Inhibitor (dpeaa)DE-He213 Biological activity (dpeaa)DE-He213 Sun, Tao verfasserin aut Wang, Tai-yi verfasserin aut Zhang, Yan verfasserin aut Liu, Hui-juan verfasserin aut Wang, Quan verfasserin aut Niu, Guo-jun verfasserin aut Liu, Wei verfasserin aut Zhou, Hong-gang verfasserin aut Yang, Cheng verfasserin aut Enthalten in Chemical Research in Chinese Universities Jilin University and The Editorial Department of Chemical Research in Chinese Universities, 2012 29(2013), 6 vom: 29. Okt., Seite 1098-1103 (DE-627)SPR03290777X nnns volume:29 year:2013 number:6 day:29 month:10 pages:1098-1103 https://dx.doi.org/10.1007/s40242-013-3216-2 lizenzpflichtig Volltext GBV_USEFLAG_A SYSFLAG_A GBV_SPRINGER SSG-OLC-PHA AR 29 2013 6 29 10 1098-1103 |
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10.1007/s40242-013-3216-2 doi (DE-627)SPR032910231 (SPR)s40242-013-3216-2-e DE-627 ger DE-627 rakwb eng Sun, Xiao-xiao verfasserin aut Synthesis and characterization of pyrazoleanthrone derivatives as Aurora A kinase inhibitors 2013 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Abstract Aurora A is a cell cycle kinase linked to cancer. For the purpose of finding biologically active of novel compounds and providing new ideas for drug-design, we performed virtual screening in commercially available databases and got pyrazoleanthrone with promising inhibitory activity against Aurora A. Optimization of solvent accessible C7 position of pyrazoleanthrone made us get thirteen target compounds. These pyrazoleanthrone derivatives were evaluated by Aurora A inhibition assays in vitro. The results show that some target compounds could inhibit Aurora A kinase. Meanwhile, these title compounds were tested in vitro against hepatocellular carcinoma(HepG2) cells by the 3′-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide(MTT) method, showing that most of them had inhibitory potency. The inhibition rate of compound 6h was about 80% against HepG2 cells, and the $ IC_{50} $ value was 17.4 μmol/L, which would be considered for further study. Pyrazoleanthrone (dpeaa)DE-He213 Aurora-A kinase (dpeaa)DE-He213 Inhibitor (dpeaa)DE-He213 Biological activity (dpeaa)DE-He213 Sun, Tao verfasserin aut Wang, Tai-yi verfasserin aut Zhang, Yan verfasserin aut Liu, Hui-juan verfasserin aut Wang, Quan verfasserin aut Niu, Guo-jun verfasserin aut Liu, Wei verfasserin aut Zhou, Hong-gang verfasserin aut Yang, Cheng verfasserin aut Enthalten in Chemical Research in Chinese Universities Jilin University and The Editorial Department of Chemical Research in Chinese Universities, 2012 29(2013), 6 vom: 29. Okt., Seite 1098-1103 (DE-627)SPR03290777X nnns volume:29 year:2013 number:6 day:29 month:10 pages:1098-1103 https://dx.doi.org/10.1007/s40242-013-3216-2 lizenzpflichtig Volltext GBV_USEFLAG_A SYSFLAG_A GBV_SPRINGER SSG-OLC-PHA AR 29 2013 6 29 10 1098-1103 |
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Elektronische Aufsätze |
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Sun, Xiao-xiao |
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10.1007/s40242-013-3216-2 |
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verfasserin |
| title_sort |
synthesis and characterization of pyrazoleanthrone derivatives as aurora a kinase inhibitors |
| title_auth |
Synthesis and characterization of pyrazoleanthrone derivatives as Aurora A kinase inhibitors |
| abstract |
Abstract Aurora A is a cell cycle kinase linked to cancer. For the purpose of finding biologically active of novel compounds and providing new ideas for drug-design, we performed virtual screening in commercially available databases and got pyrazoleanthrone with promising inhibitory activity against Aurora A. Optimization of solvent accessible C7 position of pyrazoleanthrone made us get thirteen target compounds. These pyrazoleanthrone derivatives were evaluated by Aurora A inhibition assays in vitro. The results show that some target compounds could inhibit Aurora A kinase. Meanwhile, these title compounds were tested in vitro against hepatocellular carcinoma(HepG2) cells by the 3′-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide(MTT) method, showing that most of them had inhibitory potency. The inhibition rate of compound 6h was about 80% against HepG2 cells, and the $ IC_{50} $ value was 17.4 μmol/L, which would be considered for further study. |
| abstractGer |
Abstract Aurora A is a cell cycle kinase linked to cancer. For the purpose of finding biologically active of novel compounds and providing new ideas for drug-design, we performed virtual screening in commercially available databases and got pyrazoleanthrone with promising inhibitory activity against Aurora A. Optimization of solvent accessible C7 position of pyrazoleanthrone made us get thirteen target compounds. These pyrazoleanthrone derivatives were evaluated by Aurora A inhibition assays in vitro. The results show that some target compounds could inhibit Aurora A kinase. Meanwhile, these title compounds were tested in vitro against hepatocellular carcinoma(HepG2) cells by the 3′-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide(MTT) method, showing that most of them had inhibitory potency. The inhibition rate of compound 6h was about 80% against HepG2 cells, and the $ IC_{50} $ value was 17.4 μmol/L, which would be considered for further study. |
| abstract_unstemmed |
Abstract Aurora A is a cell cycle kinase linked to cancer. For the purpose of finding biologically active of novel compounds and providing new ideas for drug-design, we performed virtual screening in commercially available databases and got pyrazoleanthrone with promising inhibitory activity against Aurora A. Optimization of solvent accessible C7 position of pyrazoleanthrone made us get thirteen target compounds. These pyrazoleanthrone derivatives were evaluated by Aurora A inhibition assays in vitro. The results show that some target compounds could inhibit Aurora A kinase. Meanwhile, these title compounds were tested in vitro against hepatocellular carcinoma(HepG2) cells by the 3′-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide(MTT) method, showing that most of them had inhibitory potency. The inhibition rate of compound 6h was about 80% against HepG2 cells, and the $ IC_{50} $ value was 17.4 μmol/L, which would be considered for further study. |
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Synthesis and characterization of pyrazoleanthrone derivatives as Aurora A kinase inhibitors |
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https://dx.doi.org/10.1007/s40242-013-3216-2 |
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Sun, Tao Wang, Tai-yi Zhang, Yan Liu, Hui-juan Wang, Quan Niu, Guo-jun Liu, Wei Zhou, Hong-gang Yang, Cheng |
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Sun, Tao Wang, Tai-yi Zhang, Yan Liu, Hui-juan Wang, Quan Niu, Guo-jun Liu, Wei Zhou, Hong-gang Yang, Cheng |
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2024-07-03T15:24:44.720Z |
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