Synthesis and Biological Evaluation of Chromenylurea and Chromanylurea Derivatives as Anti-TNF-α agents that Target the p38 MAPK Pathway
A series of 1-aryl-3-(2H-chromen-5-yl)urea and 1-aryl-3-(chroman-5-yl)urea derivatives were designed, synthesized and evaluated for their inhibitory activities towards TNF-α production in lipopolysaccharide-stimulated THP-1 cells. The most active compound, 40g, inhibited TNF-α release with an IC50 v...
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MDPI AG
2014-02-01
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| Series: | Molecules |
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| Online Access: | http://www.mdpi.com/1420-3049/19/2/2004 |
| _version_ | 1818128977484578816 |
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| author | Xingzhou Li Xinming Zhou Jing Zhang Lili Wang Long Long Zhibing Zheng Song Li Wu Zhong |
| author_facet | Xingzhou Li Xinming Zhou Jing Zhang Lili Wang Long Long Zhibing Zheng Song Li Wu Zhong |
| author_sort | Xingzhou Li |
| collection | DOAJ |
| description | A series of 1-aryl-3-(2H-chromen-5-yl)urea and 1-aryl-3-(chroman-5-yl)urea derivatives were designed, synthesized and evaluated for their inhibitory activities towards TNF-α production in lipopolysaccharide-stimulated THP-1 cells. The most active compound, 40g, inhibited TNF-α release with an IC50 value of 0.033 μM, which is equipotent to that of BIRB796 (IC50 = 0.032 μM). |
| first_indexed | 2024-12-11T07:41:49Z |
| format | Article |
| id | doaj.art-55e77faff52144d4a241a4565a8c4095 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-12-11T07:41:49Z |
| publishDate | 2014-02-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-55e77faff52144d4a241a4565a8c40952022-12-22T01:15:33ZengMDPI AGMolecules1420-30492014-02-011922004202810.3390/molecules19022004molecules19022004Synthesis and Biological Evaluation of Chromenylurea and Chromanylurea Derivatives as Anti-TNF-α agents that Target the p38 MAPK PathwayXingzhou Li0Xinming Zhou1Jing Zhang2Lili Wang3Long Long4Zhibing Zheng5Song Li6Wu Zhong7Laboratory of Computer-Aided Drug Design & Discovery, Beijing Institute of Pharmacology and Toxicology, 27 Taiping Road, Beijing 100850, ChinaLaboratory of Computer-Aided Drug Design & Discovery, Beijing Institute of Pharmacology and Toxicology, 27 Taiping Road, Beijing 100850, ChinaLaboratory of Computer-Aided Drug Design & Discovery, Beijing Institute of Pharmacology and Toxicology, 27 Taiping Road, Beijing 100850, ChinaLaboratory of Computer-Aided Drug Design & Discovery, Beijing Institute of Pharmacology and Toxicology, 27 Taiping Road, Beijing 100850, ChinaLaboratory of Computer-Aided Drug Design & Discovery, Beijing Institute of Pharmacology and Toxicology, 27 Taiping Road, Beijing 100850, ChinaLaboratory of Computer-Aided Drug Design & Discovery, Beijing Institute of Pharmacology and Toxicology, 27 Taiping Road, Beijing 100850, ChinaLaboratory of Computer-Aided Drug Design & Discovery, Beijing Institute of Pharmacology and Toxicology, 27 Taiping Road, Beijing 100850, ChinaLaboratory of Computer-Aided Drug Design & Discovery, Beijing Institute of Pharmacology and Toxicology, 27 Taiping Road, Beijing 100850, ChinaA series of 1-aryl-3-(2H-chromen-5-yl)urea and 1-aryl-3-(chroman-5-yl)urea derivatives were designed, synthesized and evaluated for their inhibitory activities towards TNF-α production in lipopolysaccharide-stimulated THP-1 cells. The most active compound, 40g, inhibited TNF-α release with an IC50 value of 0.033 μM, which is equipotent to that of BIRB796 (IC50 = 0.032 μM).http://www.mdpi.com/1420-3049/19/2/2004kinase inhibitorp38 MAPK2H-chromenylureachromanyl-urea |
| spellingShingle | Xingzhou Li Xinming Zhou Jing Zhang Lili Wang Long Long Zhibing Zheng Song Li Wu Zhong Synthesis and Biological Evaluation of Chromenylurea and Chromanylurea Derivatives as Anti-TNF-α agents that Target the p38 MAPK Pathway Molecules kinase inhibitor p38 MAPK 2H-chromenylurea chromanyl-urea |
| title | Synthesis and Biological Evaluation of Chromenylurea and Chromanylurea Derivatives as Anti-TNF-α agents that Target the p38 MAPK Pathway |
| title_full | Synthesis and Biological Evaluation of Chromenylurea and Chromanylurea Derivatives as Anti-TNF-α agents that Target the p38 MAPK Pathway |
| title_fullStr | Synthesis and Biological Evaluation of Chromenylurea and Chromanylurea Derivatives as Anti-TNF-α agents that Target the p38 MAPK Pathway |
| title_full_unstemmed | Synthesis and Biological Evaluation of Chromenylurea and Chromanylurea Derivatives as Anti-TNF-α agents that Target the p38 MAPK Pathway |
| title_short | Synthesis and Biological Evaluation of Chromenylurea and Chromanylurea Derivatives as Anti-TNF-α agents that Target the p38 MAPK Pathway |
| title_sort | synthesis and biological evaluation of chromenylurea and chromanylurea derivatives as anti tnf α agents that target the p38 mapk pathway |
| topic | kinase inhibitor p38 MAPK 2H-chromenylurea chromanyl-urea |
| url | http://www.mdpi.com/1420-3049/19/2/2004 |
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