Synthesis and biological evaluation of trisubstituted imidazole derivatives as inhibitors of p38α mitogen-activated protein kinase
A series of trisubstituted imidazole derivatives containing a 4-fluorophenyl group, a pyrimidine ring, and a CN- or CONH 2-substituted benzyl moiety have been synthesized and evaluated for p38α MAP kinase inhibitory activity. Among them, compounds 22c, 27b, and 28b inhibited p38α MAP kinase with IC...
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Veröffentlicht in: | Bioorganic & medicinal chemistry 2008-07, Vol.18 (14), p.4006-4010 |
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container_title | Bioorganic & medicinal chemistry |
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creator | Kim, Dae-Kee Lim, Jin-Hwi Lee, Jung A. Dewang, Purushottam M. |
description | A series of trisubstituted imidazole derivatives containing a 4-fluorophenyl group, a pyrimidine ring, and a CN- or CONH
2-substituted benzyl moiety have been synthesized and evaluated for p38α MAP kinase inhibitory activity. Among them, compounds
22c,
27b, and
28b inhibited p38α MAP kinase with IC
50 values 27.6, 28, and 31
nM, respectively. |
doi_str_mv | 10.1016/j.bmcl.2008.06.007 |
format | Article |
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2-substituted benzyl moiety have been synthesized and evaluated for p38α MAP kinase inhibitory activity. Among them, compounds
22c,
27b, and
28b inhibited p38α MAP kinase with IC
50 values 27.6, 28, and 31
nM, respectively.</description><identifier>ISSN: 0960-894X</identifier><identifier>ISSN: 0968-0896</identifier><identifier>EISSN: 1464-3405</identifier><identifier>EISSN: 1464-3391</identifier><identifier>DOI: 10.1016/j.bmcl.2008.06.007</identifier><language>eng</language><publisher>Elsevier Ltd</publisher><subject>Antiinflammatory ; p38α MAP kinase inhibitors ; Trisubstituted imidazole</subject><ispartof>Bioorganic & medicinal chemistry, 2008-07, Vol.18 (14), p.4006-4010</ispartof><rights>2008 Elsevier Ltd</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c331t-e7ae68cf96d63dd642b2b81ebf3e2911e4ed366cad2ae7b05a2c604c50add72d3</citedby><cites>FETCH-LOGICAL-c331t-e7ae68cf96d63dd642b2b81ebf3e2911e4ed366cad2ae7b05a2c604c50add72d3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.bmcl.2008.06.007$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>315,781,785,3551,27928,27929,45999</link.rule.ids></links><search><creatorcontrib>Kim, Dae-Kee</creatorcontrib><creatorcontrib>Lim, Jin-Hwi</creatorcontrib><creatorcontrib>Lee, Jung A.</creatorcontrib><creatorcontrib>Dewang, Purushottam M.</creatorcontrib><title>Synthesis and biological evaluation of trisubstituted imidazole derivatives as inhibitors of p38α mitogen-activated protein kinase</title><title>Bioorganic & medicinal chemistry</title><description>A series of trisubstituted imidazole derivatives containing a 4-fluorophenyl group, a pyrimidine ring, and a CN- or CONH
2-substituted benzyl moiety have been synthesized and evaluated for p38α MAP kinase inhibitory activity. Among them, compounds
22c,
27b, and
28b inhibited p38α MAP kinase with IC
50 values 27.6, 28, and 31
nM, respectively.</description><subject>Antiinflammatory</subject><subject>p38α MAP kinase inhibitors</subject><subject>Trisubstituted imidazole</subject><issn>0960-894X</issn><issn>0968-0896</issn><issn>1464-3405</issn><issn>1464-3391</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2008</creationdate><recordtype>article</recordtype><recordid>eNp9kM-KFDEQhxtRcFx9AU85eeu28mcy3eBFFl2FBQ8qeAvppHq3xu5kTNID69Un8kV8JtOMZ09Fwe_7FfU1zUsOHQeuXx-7cXFzJwD6DnQHcHjU7LjSqpUK9o-bHQwa2n5Q3542z3I-AnAFSu2aX58fQrnHTJnZ4NlIcY535OzM8Gzn1RaKgcWJlUR5HXOhshb0jBby9meckXlMdK6xM9aGzCjc00glprxRJ9n_-c2Wut9haK0rW7TipxQLUmDfKdiMz5snk50zvvg3r5qv7999uf7Q3n66-Xj99rZ1UvLS4sGi7t00aK-l91qJUYw9x3GSKAbOUaGXWjvrhcXDCHsrnAbl9mC9Pwgvr5pXl956_seKuZiFssN5tgHjmg0fpBT7QdeguARdijknnMwp0WLTg-FgNt_maDbfZvNtQJvqu0JvLhDWF86EyWRHGBx6SuiK8ZH-h_8FEImO8g</recordid><startdate>20080715</startdate><enddate>20080715</enddate><creator>Kim, Dae-Kee</creator><creator>Lim, Jin-Hwi</creator><creator>Lee, Jung A.</creator><creator>Dewang, Purushottam M.</creator><general>Elsevier Ltd</general><scope>AAYXX</scope><scope>CITATION</scope><scope>7QO</scope><scope>8FD</scope><scope>FR3</scope><scope>P64</scope></search><sort><creationdate>20080715</creationdate><title>Synthesis and biological evaluation of trisubstituted imidazole derivatives as inhibitors of p38α mitogen-activated protein kinase</title><author>Kim, Dae-Kee ; Lim, Jin-Hwi ; Lee, Jung A. ; Dewang, Purushottam M.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c331t-e7ae68cf96d63dd642b2b81ebf3e2911e4ed366cad2ae7b05a2c604c50add72d3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2008</creationdate><topic>Antiinflammatory</topic><topic>p38α MAP kinase inhibitors</topic><topic>Trisubstituted imidazole</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Kim, Dae-Kee</creatorcontrib><creatorcontrib>Lim, Jin-Hwi</creatorcontrib><creatorcontrib>Lee, Jung A.</creatorcontrib><creatorcontrib>Dewang, Purushottam M.</creatorcontrib><collection>CrossRef</collection><collection>Biotechnology Research Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><jtitle>Bioorganic & medicinal chemistry</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Kim, Dae-Kee</au><au>Lim, Jin-Hwi</au><au>Lee, Jung A.</au><au>Dewang, Purushottam M.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Synthesis and biological evaluation of trisubstituted imidazole derivatives as inhibitors of p38α mitogen-activated protein kinase</atitle><jtitle>Bioorganic & medicinal chemistry</jtitle><date>2008-07-15</date><risdate>2008</risdate><volume>18</volume><issue>14</issue><spage>4006</spage><epage>4010</epage><pages>4006-4010</pages><issn>0960-894X</issn><issn>0968-0896</issn><eissn>1464-3405</eissn><eissn>1464-3391</eissn><abstract>A series of trisubstituted imidazole derivatives containing a 4-fluorophenyl group, a pyrimidine ring, and a CN- or CONH
2-substituted benzyl moiety have been synthesized and evaluated for p38α MAP kinase inhibitory activity. Among them, compounds
22c,
27b, and
28b inhibited p38α MAP kinase with IC
50 values 27.6, 28, and 31
nM, respectively.</abstract><pub>Elsevier Ltd</pub><doi>10.1016/j.bmcl.2008.06.007</doi><tpages>5</tpages></addata></record> |
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subjects | Antiinflammatory p38α MAP kinase inhibitors Trisubstituted imidazole |
title | Synthesis and biological evaluation of trisubstituted imidazole derivatives as inhibitors of p38α mitogen-activated protein kinase |
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