Identification of 3-amido-4-anilinoquinolines as potent and selective inhibitors of CSF-1R kinase
3-Amido-4-anilinoquinolines are potent and highly selective inhibitors of CSF-1R. Their synthesis and SAR is reported, along with initial efforts to optimize the physical properties and PK through modifications at the quinoline 6- and 7-positions.
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2009-02, Vol.19 (3), p.697-700 |
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| container_title | Bioorganic & medicinal chemistry letters |
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| creator | Scott, David A. Balliet, Carrie L. Cook, Donald J. Davies, Audrey M. Gero, Thomas W. Omer, Charles A. Poondru, Srinivasu Theoclitou, Maria-Elena Tyurin, Boris Zinda, Michael J. |
| description | 3-Amido-4-anilinoquinolines are potent and highly selective inhibitors of CSF-1R. Their synthesis and SAR is reported, along with initial efforts to optimize the physical properties and PK through modifications at the quinoline 6- and 7-positions. |
| doi_str_mv | 10.1016/j.bmcl.2008.12.046 |
| format | Article |
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Drug treatments ; Protein Kinase Inhibitors - chemical synthesis ; Protein Kinase Inhibitors - chemistry ; Quinoline ; Quinolines - chemistry ; Quinolines - pharmacokinetics ; Rats ; Receptor, Macrophage Colony-Stimulating Factor - antagonists & inhibitors ; Receptor, Macrophage Colony-Stimulating Factor - chemistry</subject><ispartof>Bioorganic & medicinal chemistry letters, 2009-02, Vol.19 (3), p.697-700</ispartof><rights>2008 Elsevier Ltd</rights><rights>2009 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c416t-26c795677eca9286c69facd45f420cf59efefe5fa7ba7c55d9e1e35355b11b0b3</citedby><cites>FETCH-LOGICAL-c416t-26c795677eca9286c69facd45f420cf59efefe5fa7ba7c55d9e1e35355b11b0b3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0960894X08015564$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3537,27901,27902,65306</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=21123396$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/19112018$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Scott, David A.</creatorcontrib><creatorcontrib>Balliet, Carrie L.</creatorcontrib><creatorcontrib>Cook, Donald J.</creatorcontrib><creatorcontrib>Davies, Audrey M.</creatorcontrib><creatorcontrib>Gero, Thomas W.</creatorcontrib><creatorcontrib>Omer, Charles A.</creatorcontrib><creatorcontrib>Poondru, Srinivasu</creatorcontrib><creatorcontrib>Theoclitou, Maria-Elena</creatorcontrib><creatorcontrib>Tyurin, Boris</creatorcontrib><creatorcontrib>Zinda, Michael J.</creatorcontrib><title>Identification of 3-amido-4-anilinoquinolines as potent and selective inhibitors of CSF-1R kinase</title><title>Bioorganic & medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>3-Amido-4-anilinoquinolines are potent and highly selective inhibitors of CSF-1R. Their synthesis and SAR is reported, along with initial efforts to optimize the physical properties and PK through modifications at the quinoline 6- and 7-positions.</description><subject>Administration, Oral</subject><subject>Animals</subject><subject>Antineoplastic agents</subject><subject>Antineoplastic Agents - chemical synthesis</subject><subject>Antineoplastic Agents - chemistry</subject><subject>Biological and medical sciences</subject><subject>Chemistry, Pharmaceutical - methods</subject><subject>CSF-1R</subject><subject>Drug Design</subject><subject>General aspects</subject><subject>Humans</subject><subject>Inhibitory Concentration 50</subject><subject>Kinase inhibitor</subject><subject>Kinetics</subject><subject>Medical sciences</subject><subject>Models, Chemical</subject><subject>Neoplasms - drug therapy</subject><subject>Pharmacology. Drug treatments</subject><subject>Protein Kinase Inhibitors - chemical synthesis</subject><subject>Protein Kinase Inhibitors - chemistry</subject><subject>Quinoline</subject><subject>Quinolines - chemistry</subject><subject>Quinolines - pharmacokinetics</subject><subject>Rats</subject><subject>Receptor, Macrophage Colony-Stimulating Factor - antagonists & inhibitors</subject><subject>Receptor, Macrophage Colony-Stimulating Factor - chemistry</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2009</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kU9rFTEUxYNY7LP6BVzIbNTVTPM_E3BTHrYWCoWq4C5kMjeY50zyTOYV_PZmeI-6Kxdys_idw-UchN4R3BFM5OWuG2Y3dRTjviO0w1y-QBvCJW8Zx-Il2mAtcdtr_vMcvS5lhzHhmPNX6JxoQigm_QbZ2xHiEnxwdgkpNsk3rLVzGFPLWxvDFGL6c6hP_UBpbGn2aamKxsaxKTCBW8IjNCH-CkNYUi6rw_bbdUsemt8h2gJv0Jm3U4G3p32Bflx_-b792t7d39xur-5ax4lcWiqd0kIqBc5q2ksntbdu5MJzip0XGnwd4a0arHJCjBoIMMGEGAgZ8MAu0Kej7z7Xi6EsZg7FwTTZCOlQjGJMMiKUqOTHZ0mKGe17pSpIj6DLqZQM3uxzmG3-awg2awVmZ9YKzFqBIdTUCqro_cn9MMww_pecMq_AhxNgi7OTzza6UJ44WjHG9Gr0-chBTe0xQDbFBYgOxpBr7GZM4bk7_gGjRqTE</recordid><startdate>20090201</startdate><enddate>20090201</enddate><creator>Scott, David A.</creator><creator>Balliet, Carrie L.</creator><creator>Cook, Donald J.</creator><creator>Davies, Audrey M.</creator><creator>Gero, Thomas W.</creator><creator>Omer, Charles A.</creator><creator>Poondru, Srinivasu</creator><creator>Theoclitou, Maria-Elena</creator><creator>Tyurin, Boris</creator><creator>Zinda, Michael J.</creator><general>Elsevier Ltd</general><general>Elsevier</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7QO</scope><scope>8FD</scope><scope>FR3</scope><scope>P64</scope><scope>7X8</scope></search><sort><creationdate>20090201</creationdate><title>Identification of 3-amido-4-anilinoquinolines as potent and selective inhibitors of CSF-1R kinase</title><author>Scott, David A. ; Balliet, Carrie L. ; Cook, Donald J. ; Davies, Audrey M. ; Gero, Thomas W. ; Omer, Charles A. ; Poondru, Srinivasu ; Theoclitou, Maria-Elena ; Tyurin, Boris ; Zinda, Michael J.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c416t-26c795677eca9286c69facd45f420cf59efefe5fa7ba7c55d9e1e35355b11b0b3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2009</creationdate><topic>Administration, Oral</topic><topic>Animals</topic><topic>Antineoplastic agents</topic><topic>Antineoplastic Agents - chemical synthesis</topic><topic>Antineoplastic Agents - chemistry</topic><topic>Biological and medical sciences</topic><topic>Chemistry, Pharmaceutical - methods</topic><topic>CSF-1R</topic><topic>Drug Design</topic><topic>General aspects</topic><topic>Humans</topic><topic>Inhibitory Concentration 50</topic><topic>Kinase inhibitor</topic><topic>Kinetics</topic><topic>Medical sciences</topic><topic>Models, Chemical</topic><topic>Neoplasms - drug therapy</topic><topic>Pharmacology. Drug treatments</topic><topic>Protein Kinase Inhibitors - chemical synthesis</topic><topic>Protein Kinase Inhibitors - chemistry</topic><topic>Quinoline</topic><topic>Quinolines - chemistry</topic><topic>Quinolines - pharmacokinetics</topic><topic>Rats</topic><topic>Receptor, Macrophage Colony-Stimulating Factor - antagonists & inhibitors</topic><topic>Receptor, Macrophage Colony-Stimulating Factor - chemistry</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Scott, David A.</creatorcontrib><creatorcontrib>Balliet, Carrie L.</creatorcontrib><creatorcontrib>Cook, Donald J.</creatorcontrib><creatorcontrib>Davies, Audrey M.</creatorcontrib><creatorcontrib>Gero, Thomas W.</creatorcontrib><creatorcontrib>Omer, Charles A.</creatorcontrib><creatorcontrib>Poondru, Srinivasu</creatorcontrib><creatorcontrib>Theoclitou, Maria-Elena</creatorcontrib><creatorcontrib>Tyurin, Boris</creatorcontrib><creatorcontrib>Zinda, Michael 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>Scott, David A.</au><au>Balliet, Carrie L.</au><au>Cook, Donald J.</au><au>Davies, Audrey M.</au><au>Gero, Thomas W.</au><au>Omer, Charles A.</au><au>Poondru, Srinivasu</au><au>Theoclitou, Maria-Elena</au><au>Tyurin, Boris</au><au>Zinda, Michael J.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Identification of 3-amido-4-anilinoquinolines as potent and selective inhibitors of CSF-1R kinase</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2009-02-01</date><risdate>2009</risdate><volume>19</volume><issue>3</issue><spage>697</spage><epage>700</epage><pages>697-700</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>3-Amido-4-anilinoquinolines are potent and highly selective inhibitors of CSF-1R. Their synthesis and SAR is reported, along with initial efforts to optimize the physical properties and PK through modifications at the quinoline 6- and 7-positions.</abstract><cop>Amsterdam</cop><pub>Elsevier Ltd</pub><pmid>19112018</pmid><doi>10.1016/j.bmcl.2008.12.046</doi><tpages>4</tpages></addata></record> |
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| ispartof | Bioorganic & medicinal chemistry letters, 2009-02, Vol.19 (3), p.697-700 |
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| language | eng |
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| source | MEDLINE; ScienceDirect Journals (5 years ago - present) |
| subjects | Administration, Oral Animals Antineoplastic agents Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Biological and medical sciences Chemistry, Pharmaceutical - methods CSF-1R Drug Design General aspects Humans Inhibitory Concentration 50 Kinase inhibitor Kinetics Medical sciences Models, Chemical Neoplasms - drug therapy Pharmacology. Drug treatments Protein Kinase Inhibitors - chemical synthesis Protein Kinase Inhibitors - chemistry Quinoline Quinolines - chemistry Quinolines - pharmacokinetics Rats Receptor, Macrophage Colony-Stimulating Factor - antagonists & inhibitors Receptor, Macrophage Colony-Stimulating Factor - chemistry |
| title | Identification of 3-amido-4-anilinoquinolines as potent and selective inhibitors of CSF-1R kinase |
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