Synthesis and inhibition of PGE2 production of 6,8-disubstituted chrysin derivatives
A series of 6,8-disubstituted chrysin derivatives have been synthesized and evaluated for their PGE2 inhibitory activities. 6,8-Disubstituted chrysin derivatives were obtained from naturally occurring chrysin by halogenation, oxidation, thiomethylation and C-C cross coupling reaction. Among the comp...
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| Veröffentlicht in: | European journal of medicinal chemistry 2005-09, Vol.40 (9), p.943-948 |
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| container_title | European journal of medicinal chemistry |
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| creator | PARK, Haeil TRAN THANH DAO HYUN PYO KIM |
| description | A series of 6,8-disubstituted chrysin derivatives have been synthesized and evaluated for their PGE2 inhibitory activities. 6,8-Disubstituted chrysin derivatives were obtained from naturally occurring chrysin by halogenation, oxidation, thiomethylation and C-C cross coupling reaction. Among the compounds investigated, 6,8-dibromochrysin (2), 6,8-diiodochrysin (4), 6,8-dimethylthiochrysin (9) and 6,8-dimethoxychrysin (11) showed as strong inhibitory activities of PGE2 production from LPS-induced RAW 264.7 cells as wogonin, a well known natural flavone having strong and selective COX-2 inhibitory activity. |
| doi_str_mv | 10.1016/j.ejmech.2005.04.013 |
| format | Article |
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Among the compounds investigated, 6,8-dibromochrysin (2), 6,8-diiodochrysin (4), 6,8-dimethylthiochrysin (9) and 6,8-dimethoxychrysin (11) showed as strong inhibitory activities of PGE2 production from LPS-induced RAW 264.7 cells as wogonin, a well known natural flavone having strong and selective COX-2 inhibitory activity.</description><identifier>ISSN: 0223-5234</identifier><identifier>EISSN: 1768-3254</identifier><identifier>DOI: 10.1016/j.ejmech.2005.04.013</identifier><identifier>PMID: 15963606</identifier><identifier>CODEN: EJMCA5</identifier><language>eng</language><publisher>Oxford: Elsevier</publisher><subject>Animals ; Biological and medical sciences ; Bones, joints and connective tissue. 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Among the compounds investigated, 6,8-dibromochrysin (2), 6,8-diiodochrysin (4), 6,8-dimethylthiochrysin (9) and 6,8-dimethoxychrysin (11) showed as strong inhibitory activities of PGE2 production from LPS-induced RAW 264.7 cells as wogonin, a well known natural flavone having strong and selective COX-2 inhibitory activity.</description><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>Bones, joints and connective tissue. Antiinflammatory agents</subject><subject>Cell Line</subject><subject>Cyclooxygenase 2 Inhibitors - chemical synthesis</subject><subject>Cyclooxygenase 2 Inhibitors - pharmacology</subject><subject>Dinoprostone - antagonists & inhibitors</subject><subject>Dinoprostone - metabolism</subject><subject>Drug Evaluation, Preclinical</subject><subject>Flavonoids - chemical synthesis</subject><subject>Flavonoids - chemistry</subject><subject>Flavonoids - pharmacology</subject><subject>Macrophages - drug effects</subject><subject>Medical sciences</subject><subject>Mice</subject><subject>Molecular Structure</subject><subject>Pharmacology. 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Antiinflammatory agents</topic><topic>Cell Line</topic><topic>Cyclooxygenase 2 Inhibitors - chemical synthesis</topic><topic>Cyclooxygenase 2 Inhibitors - pharmacology</topic><topic>Dinoprostone - antagonists & inhibitors</topic><topic>Dinoprostone - metabolism</topic><topic>Drug Evaluation, Preclinical</topic><topic>Flavonoids - chemical synthesis</topic><topic>Flavonoids - chemistry</topic><topic>Flavonoids - pharmacology</topic><topic>Macrophages - drug effects</topic><topic>Medical sciences</topic><topic>Mice</topic><topic>Molecular Structure</topic><topic>Pharmacology. Drug treatments</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>PARK, Haeil</creatorcontrib><creatorcontrib>TRAN THANH DAO</creatorcontrib><creatorcontrib>HYUN PYO KIM</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>MEDLINE - Academic</collection><jtitle>European journal of medicinal chemistry</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>PARK, Haeil</au><au>TRAN THANH DAO</au><au>HYUN PYO KIM</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Synthesis and inhibition of PGE2 production of 6,8-disubstituted chrysin derivatives</atitle><jtitle>European journal of medicinal chemistry</jtitle><addtitle>Eur J Med Chem</addtitle><date>2005-09</date><risdate>2005</risdate><volume>40</volume><issue>9</issue><spage>943</spage><epage>948</epage><pages>943-948</pages><issn>0223-5234</issn><eissn>1768-3254</eissn><coden>EJMCA5</coden><abstract>A series of 6,8-disubstituted chrysin derivatives have been synthesized and evaluated for their PGE2 inhibitory activities. 6,8-Disubstituted chrysin derivatives were obtained from naturally occurring chrysin by halogenation, oxidation, thiomethylation and C-C cross coupling reaction. 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| ispartof | European journal of medicinal chemistry, 2005-09, Vol.40 (9), p.943-948 |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Animals Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Cell Line Cyclooxygenase 2 Inhibitors - chemical synthesis Cyclooxygenase 2 Inhibitors - pharmacology Dinoprostone - antagonists & inhibitors Dinoprostone - metabolism Drug Evaluation, Preclinical Flavonoids - chemical synthesis Flavonoids - chemistry Flavonoids - pharmacology Macrophages - drug effects Medical sciences Mice Molecular Structure Pharmacology. Drug treatments |
| title | Synthesis and inhibition of PGE2 production of 6,8-disubstituted chrysin derivatives |
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