Novel non-benzimidazole chk2 kinase inhibitors
A number of benzimidazole replacements were synthesized and examined to gain a greater understanding of the SAR around this novel series of chk2 kinase inhibitors. In a recent paper, [Arienti, K. L.; Brunmark, A.; Axe, F. U.; McClure, K. M.; Lee, A.; Blevitt, J.; Neff, D. K.; Huang, L.; Crawford, S....
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2006-04, Vol.16 (7), p.1924-1928 |
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| container_issue | 7 |
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| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 16 |
| creator | McClure, Kelly J. Huang, Liming Arienti, Kristen L. Axe, Frank U. Brunmark, Anders Blevitt, Jon Guy Breitenbucher, J. |
| description | A number of benzimidazole replacements were synthesized and examined to gain a greater understanding of the SAR around this novel series of chk2 kinase inhibitors.
In a recent paper, [Arienti, K. L.; Brunmark, A.; Axe, F. U.; McClure, K. M.; Lee, A.; Blevitt, J.; Neff, D. K.; Huang, L.; Crawford, S.; Chennagiri, R. P.; Karlsson, L.; Brietenbucher, J. G.
J. Med. Chem.
2005,
48, 1873], we described the discovery of a class of benzimidazole chk2 kinase inhibitors, exemplified by compound
1, which had radio-protective effects in human T-cells subjected to ionizing radiation. Here, a series of non-benzimidazole analogs intended to define the scope of the SAR about this new series of inhibitor, and allow for refinement of the binding model of these compounds to the chk2 kinase is described. |
| doi_str_mv | 10.1016/j.bmcl.2005.12.096 |
| format | Article |
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In a recent paper, [Arienti, K. L.; Brunmark, A.; Axe, F. U.; McClure, K. M.; Lee, A.; Blevitt, J.; Neff, D. K.; Huang, L.; Crawford, S.; Chennagiri, R. P.; Karlsson, L.; Brietenbucher, J. G.
J. Med. Chem.
2005,
48, 1873], we described the discovery of a class of benzimidazole chk2 kinase inhibitors, exemplified by compound
1, which had radio-protective effects in human T-cells subjected to ionizing radiation. Here, a series of non-benzimidazole analogs intended to define the scope of the SAR about this new series of inhibitor, and allow for refinement of the binding model of these compounds to the chk2 kinase is described.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2005.12.096</identifier><identifier>PMID: 16442290</identifier><language>eng</language><publisher>Oxford: Elsevier Ltd</publisher><subject>Benzimidazoles - chemistry ; Benzimidazoles - pharmacology ; Biological and medical sciences ; Checkpoint Kinase 2 ; Medical sciences ; Miscellaneous ; Models, Molecular ; Pharmacology. Drug treatments ; Protein Kinase Inhibitors - chemistry ; Protein Kinase Inhibitors - pharmacology ; Protein-Serine-Threonine Kinases - antagonists & inhibitors ; Radiation therapy and radiosensitizing agent ; Radiation-Protective Agents - chemistry ; Radiation-Protective Agents - pharmacology ; Structure-Activity Relationship ; Treatment with physical agents ; Treatment. General aspects ; Tumors</subject><ispartof>Bioorganic & medicinal chemistry letters, 2006-04, Vol.16 (7), p.1924-1928</ispartof><rights>2006 Elsevier Ltd</rights><rights>2006 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c415t-adb25325a50b06640a8264b5ba98fbf9ceee359d6fd40bf3317a3de79dfac11b3</citedby><cites>FETCH-LOGICAL-c415t-adb25325a50b06640a8264b5ba98fbf9ceee359d6fd40bf3317a3de79dfac11b3</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.2005.12.096$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=17561107$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/16442290$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>McClure, Kelly J.</creatorcontrib><creatorcontrib>Huang, Liming</creatorcontrib><creatorcontrib>Arienti, Kristen L.</creatorcontrib><creatorcontrib>Axe, Frank U.</creatorcontrib><creatorcontrib>Brunmark, Anders</creatorcontrib><creatorcontrib>Blevitt, Jon</creatorcontrib><creatorcontrib>Guy Breitenbucher, J.</creatorcontrib><title>Novel non-benzimidazole chk2 kinase inhibitors</title><title>Bioorganic & medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>A number of benzimidazole replacements were synthesized and examined to gain a greater understanding of the SAR around this novel series of chk2 kinase inhibitors.
In a recent paper, [Arienti, K. L.; Brunmark, A.; Axe, F. U.; McClure, K. M.; Lee, A.; Blevitt, J.; Neff, D. K.; Huang, L.; Crawford, S.; Chennagiri, R. P.; Karlsson, L.; Brietenbucher, J. G.
J. Med. Chem.
2005,
48, 1873], we described the discovery of a class of benzimidazole chk2 kinase inhibitors, exemplified by compound
1, which had radio-protective effects in human T-cells subjected to ionizing radiation. Here, a series of non-benzimidazole analogs intended to define the scope of the SAR about this new series of inhibitor, and allow for refinement of the binding model of these compounds to the chk2 kinase is described.</description><subject>Benzimidazoles - chemistry</subject><subject>Benzimidazoles - pharmacology</subject><subject>Biological and medical sciences</subject><subject>Checkpoint Kinase 2</subject><subject>Medical sciences</subject><subject>Miscellaneous</subject><subject>Models, Molecular</subject><subject>Pharmacology. Drug treatments</subject><subject>Protein Kinase Inhibitors - chemistry</subject><subject>Protein Kinase Inhibitors - pharmacology</subject><subject>Protein-Serine-Threonine Kinases - antagonists & inhibitors</subject><subject>Radiation therapy and radiosensitizing agent</subject><subject>Radiation-Protective Agents - chemistry</subject><subject>Radiation-Protective Agents - pharmacology</subject><subject>Structure-Activity Relationship</subject><subject>Treatment with physical agents</subject><subject>Treatment. 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Drug treatments</topic><topic>Protein Kinase Inhibitors - chemistry</topic><topic>Protein Kinase Inhibitors - pharmacology</topic><topic>Protein-Serine-Threonine Kinases - antagonists & inhibitors</topic><topic>Radiation therapy and radiosensitizing agent</topic><topic>Radiation-Protective Agents - chemistry</topic><topic>Radiation-Protective Agents - pharmacology</topic><topic>Structure-Activity Relationship</topic><topic>Treatment with physical agents</topic><topic>Treatment. General aspects</topic><topic>Tumors</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>McClure, Kelly J.</creatorcontrib><creatorcontrib>Huang, Liming</creatorcontrib><creatorcontrib>Arienti, Kristen L.</creatorcontrib><creatorcontrib>Axe, Frank U.</creatorcontrib><creatorcontrib>Brunmark, Anders</creatorcontrib><creatorcontrib>Blevitt, Jon</creatorcontrib><creatorcontrib>Guy Breitenbucher, J.</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>CrossRef</collection><collection>Biotechnology Research Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>Bioorganic & medicinal chemistry letters</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>McClure, Kelly J.</au><au>Huang, Liming</au><au>Arienti, Kristen L.</au><au>Axe, Frank U.</au><au>Brunmark, Anders</au><au>Blevitt, Jon</au><au>Guy Breitenbucher, J.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Novel non-benzimidazole chk2 kinase inhibitors</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2006-04-01</date><risdate>2006</risdate><volume>16</volume><issue>7</issue><spage>1924</spage><epage>1928</epage><pages>1924-1928</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>A number of benzimidazole replacements were synthesized and examined to gain a greater understanding of the SAR around this novel series of chk2 kinase inhibitors.
In a recent paper, [Arienti, K. L.; Brunmark, A.; Axe, F. U.; McClure, K. M.; Lee, A.; Blevitt, J.; Neff, D. K.; Huang, L.; Crawford, S.; Chennagiri, R. P.; Karlsson, L.; Brietenbucher, J. G.
J. Med. Chem.
2005,
48, 1873], we described the discovery of a class of benzimidazole chk2 kinase inhibitors, exemplified by compound
1, which had radio-protective effects in human T-cells subjected to ionizing radiation. Here, a series of non-benzimidazole analogs intended to define the scope of the SAR about this new series of inhibitor, and allow for refinement of the binding model of these compounds to the chk2 kinase is described.</abstract><cop>Oxford</cop><pub>Elsevier Ltd</pub><pmid>16442290</pmid><doi>10.1016/j.bmcl.2005.12.096</doi><tpages>5</tpages></addata></record> |
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| subjects | Benzimidazoles - chemistry Benzimidazoles - pharmacology Biological and medical sciences Checkpoint Kinase 2 Medical sciences Miscellaneous Models, Molecular Pharmacology. Drug treatments Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacology Protein-Serine-Threonine Kinases - antagonists & inhibitors Radiation therapy and radiosensitizing agent Radiation-Protective Agents - chemistry Radiation-Protective Agents - pharmacology Structure-Activity Relationship Treatment with physical agents Treatment. General aspects Tumors |
| title | Novel non-benzimidazole chk2 kinase inhibitors |
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