Synthesis and in vitro antitumor activity of new quinoxaline derivatives
A series of novel 5,7-diamino-3-phenyl-2-benzylamino, 2-phenoxy, and 2-thiophenyl substituted quinoxalines has been designed, synthesized and evaluated for their in vitro antitumor activity towards cell lines of nine different types of human cancers. Some of these compounds exhibited inhibitory effe...
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| Veröffentlicht in: | European journal of medicinal chemistry 2009-04, Vol.44 (4), p.1579-1591 |
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| container_issue | 4 |
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| container_title | European journal of medicinal chemistry |
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| creator | Corona, Paola Carta, Antonio Loriga, Mario Vitale, Gabriella Paglietti, Giuseppe |
| description | A series of novel 5,7-diamino-3-phenyl-2-benzylamino, 2-phenoxy, and 2-thiophenyl substituted quinoxalines has been designed, synthesized and evaluated for their in vitro antitumor activity towards cell lines of nine different types of human cancers. Some of these compounds exhibited inhibitory effects on the growth of a wide range of cancer cell lines generally at 10
−6
M, in some cases at 10
−7
M and 10
−8
M concentrations. Within this series the benzylamino quinoxaline derivatives
1b–
7b were the most active, whereas compound
2c showed the highest MG_MD value (−5.66).
[Display omitted] A series of novel 5,7-diamino-3-phenyl-2-benzylamino, 2-phenoxy, and 2-thiophenyl substituted quinoxalines have been designed, synthesized and evaluated for their in vitro antitumor activity towards cell lines of nine different types of human cancers. |
| doi_str_mv | 10.1016/j.ejmech.2008.07.025 |
| format | Article |
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−6
M, in some cases at 10
−7
M and 10
−8
M concentrations. Within this series the benzylamino quinoxaline derivatives
1b–
7b were the most active, whereas compound
2c showed the highest MG_MD value (−5.66).
[Display omitted] A series of novel 5,7-diamino-3-phenyl-2-benzylamino, 2-phenoxy, and 2-thiophenyl substituted quinoxalines have been designed, synthesized and evaluated for their in vitro antitumor activity towards cell lines of nine different types of human cancers.</description><identifier>ISSN: 0223-5234</identifier><identifier>EISSN: 1768-3254</identifier><identifier>DOI: 10.1016/j.ejmech.2008.07.025</identifier><identifier>PMID: 18774202</identifier><identifier>CODEN: EJMCA5</identifier><language>eng</language><publisher>Kidlington: Elsevier Masson SAS</publisher><subject>5,7-Diamino-3-phenyl-2-benzylamino, 2-phenoxy and 2-phenylthio substituted quinoxalines ; Antineoplastic agents ; Antineoplastic Agents - chemical synthesis ; Antineoplastic Agents - chemistry ; Antineoplastic Agents - pharmacology ; Antitumor activity ; Biological and medical sciences ; Cell Line, Tumor ; Drug Design ; General aspects ; Humans ; Medical sciences ; Pharmacology. Drug treatments ; Quinoxalines - chemical synthesis ; Quinoxalines - chemistry ; Quinoxalines - pharmacology</subject><ispartof>European journal of medicinal chemistry, 2009-04, Vol.44 (4), p.1579-1591</ispartof><rights>2008 Elsevier Masson SAS</rights><rights>2009 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c390t-95c1a0fe3e78220ffa92185637b9457939401b92a43c30c728a8189c3b9c0a7a3</citedby></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0223523408003541$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3537,27901,27902,65306</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=21337729$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/18774202$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Corona, Paola</creatorcontrib><creatorcontrib>Carta, Antonio</creatorcontrib><creatorcontrib>Loriga, Mario</creatorcontrib><creatorcontrib>Vitale, Gabriella</creatorcontrib><creatorcontrib>Paglietti, Giuseppe</creatorcontrib><title>Synthesis and in vitro antitumor activity of new quinoxaline derivatives</title><title>European journal of medicinal chemistry</title><addtitle>Eur J Med Chem</addtitle><description>A series of novel 5,7-diamino-3-phenyl-2-benzylamino, 2-phenoxy, and 2-thiophenyl substituted quinoxalines has been designed, synthesized and evaluated for their in vitro antitumor activity towards cell lines of nine different types of human cancers. Some of these compounds exhibited inhibitory effects on the growth of a wide range of cancer cell lines generally at 10
−6
M, in some cases at 10
−7
M and 10
−8
M concentrations. Within this series the benzylamino quinoxaline derivatives
1b–
7b were the most active, whereas compound
2c showed the highest MG_MD value (−5.66).
[Display omitted] A series of novel 5,7-diamino-3-phenyl-2-benzylamino, 2-phenoxy, and 2-thiophenyl substituted quinoxalines have been designed, synthesized and evaluated for their in vitro antitumor activity towards cell lines of nine different types of human cancers.</description><subject>5,7-Diamino-3-phenyl-2-benzylamino, 2-phenoxy and 2-phenylthio substituted quinoxalines</subject><subject>Antineoplastic agents</subject><subject>Antineoplastic Agents - chemical synthesis</subject><subject>Antineoplastic Agents - chemistry</subject><subject>Antineoplastic Agents - pharmacology</subject><subject>Antitumor activity</subject><subject>Biological and medical sciences</subject><subject>Cell Line, Tumor</subject><subject>Drug Design</subject><subject>General aspects</subject><subject>Humans</subject><subject>Medical sciences</subject><subject>Pharmacology. Drug treatments</subject><subject>Quinoxalines - chemical synthesis</subject><subject>Quinoxalines - chemistry</subject><subject>Quinoxalines - pharmacology</subject><issn>0223-5234</issn><issn>1768-3254</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2009</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kE1LxDAQhoMoun78A5Fe9NY6SdomuQiy-AWCB_UcsukUs7SpJu3q_nsju-jN0zAzzzsMDyGnFAoKtL5cFrjs0b4VDEAWIApg1Q6ZUVHLnLOq3CUzYIznFePlATmMcQkAVQ2wTw6oFKJkwGbk_nntxzeMLmbGN5nz2cqNYUjN6MapH0Jm7OjSbJ0NbebxM_uYnB--TOc8Zg0GtzJpj_GY7LWmi3iyrUfk9fbmZX6fPz7dPcyvH3PLFYy5qiw10CJHIRmDtjWKUVnVXCxUWQnFVQl0oZgpueVgBZNGUqksXygLRhh-RC42d9_D8DFhHHXvosWuMx6HKeq6VkpVUiaw3IA2DDEGbPV7cL0Ja01B_xjUS70xqH8MahA6GUyxs-39adFj8xfaKkvA-RYw0ZquDcZbF385RjkXgqnEXW04TDZWDoOO1qG32LiAdtTN4P7_5BsU2ZBZ</recordid><startdate>20090401</startdate><enddate>20090401</enddate><creator>Corona, Paola</creator><creator>Carta, Antonio</creator><creator>Loriga, Mario</creator><creator>Vitale, Gabriella</creator><creator>Paglietti, Giuseppe</creator><general>Elsevier Masson SAS</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>7X8</scope></search><sort><creationdate>20090401</creationdate><title>Synthesis and in vitro antitumor activity of new quinoxaline derivatives</title><author>Corona, Paola ; Carta, Antonio ; Loriga, Mario ; Vitale, Gabriella ; Paglietti, Giuseppe</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c390t-95c1a0fe3e78220ffa92185637b9457939401b92a43c30c728a8189c3b9c0a7a3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2009</creationdate><topic>5,7-Diamino-3-phenyl-2-benzylamino, 2-phenoxy and 2-phenylthio substituted quinoxalines</topic><topic>Antineoplastic agents</topic><topic>Antineoplastic Agents - chemical synthesis</topic><topic>Antineoplastic Agents - chemistry</topic><topic>Antineoplastic Agents - pharmacology</topic><topic>Antitumor activity</topic><topic>Biological and medical sciences</topic><topic>Cell Line, Tumor</topic><topic>Drug Design</topic><topic>General aspects</topic><topic>Humans</topic><topic>Medical sciences</topic><topic>Pharmacology. Drug treatments</topic><topic>Quinoxalines - chemical synthesis</topic><topic>Quinoxalines - chemistry</topic><topic>Quinoxalines - pharmacology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Corona, Paola</creatorcontrib><creatorcontrib>Carta, Antonio</creatorcontrib><creatorcontrib>Loriga, Mario</creatorcontrib><creatorcontrib>Vitale, Gabriella</creatorcontrib><creatorcontrib>Paglietti, Giuseppe</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>MEDLINE - Academic</collection><jtitle>European journal of medicinal chemistry</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Corona, Paola</au><au>Carta, Antonio</au><au>Loriga, Mario</au><au>Vitale, Gabriella</au><au>Paglietti, Giuseppe</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Synthesis and in vitro antitumor activity of new quinoxaline derivatives</atitle><jtitle>European journal of medicinal chemistry</jtitle><addtitle>Eur J Med Chem</addtitle><date>2009-04-01</date><risdate>2009</risdate><volume>44</volume><issue>4</issue><spage>1579</spage><epage>1591</epage><pages>1579-1591</pages><issn>0223-5234</issn><eissn>1768-3254</eissn><coden>EJMCA5</coden><abstract>A series of novel 5,7-diamino-3-phenyl-2-benzylamino, 2-phenoxy, and 2-thiophenyl substituted quinoxalines has been designed, synthesized and evaluated for their in vitro antitumor activity towards cell lines of nine different types of human cancers. Some of these compounds exhibited inhibitory effects on the growth of a wide range of cancer cell lines generally at 10
−6
M, in some cases at 10
−7
M and 10
−8
M concentrations. Within this series the benzylamino quinoxaline derivatives
1b–
7b were the most active, whereas compound
2c showed the highest MG_MD value (−5.66).
[Display omitted] A series of novel 5,7-diamino-3-phenyl-2-benzylamino, 2-phenoxy, and 2-thiophenyl substituted quinoxalines have been designed, synthesized and evaluated for their in vitro antitumor activity towards cell lines of nine different types of human cancers.</abstract><cop>Kidlington</cop><pub>Elsevier Masson SAS</pub><pmid>18774202</pmid><doi>10.1016/j.ejmech.2008.07.025</doi><tpages>13</tpages></addata></record> |
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| ispartof | European journal of medicinal chemistry, 2009-04, Vol.44 (4), p.1579-1591 |
| issn | 0223-5234 1768-3254 |
| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | 5,7-Diamino-3-phenyl-2-benzylamino, 2-phenoxy and 2-phenylthio substituted quinoxalines Antineoplastic agents Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Antitumor activity Biological and medical sciences Cell Line, Tumor Drug Design General aspects Humans Medical sciences Pharmacology. Drug treatments Quinoxalines - chemical synthesis Quinoxalines - chemistry Quinoxalines - pharmacology |
| title | Synthesis and in vitro antitumor activity of new quinoxaline derivatives |
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