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5-Imidazolyl-quinolinones, -quinazolinones and -benzo-azepinones as farnesyltransferase inhibitors
The evaluation of structure–activity relationships associated with the modification of the R115777 quinolinone ring moiety displaying potent in vitro inhibiting activity is described. The synthesis and inhibiting potency of farnesyltransferase inhibitors closely related to R115777 is reported.
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| Published in: | Bioorganic & medicinal chemistry letters 2003-05, Vol.13 (9), p.1543-1547 |
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| Main Authors: | , , , , , , , , , , , , , , , |
| Format: | Article |
| Language: | English |
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| cited_by | cdi_FETCH-LOGICAL-c393t-15c3f6e51e52e8b6c6d72bcf15ba9c3594c3ab9d97e7e83fba3b5aa068d874c53 |
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| cites | cdi_FETCH-LOGICAL-c393t-15c3f6e51e52e8b6c6d72bcf15ba9c3594c3ab9d97e7e83fba3b5aa068d874c53 |
| container_end_page | 1547 |
| container_issue | 9 |
| container_start_page | 1543 |
| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 13 |
| creator | Angibaud, Patrick Bourdrez, Xavier Devine, Ann End, David W Freyne, Eddy Ligny, Yannick Muller, Philippe Mannens, Geert Pilatte, Isabelle Poncelet, Virginie Skrzat, Stacy Smets, Gerda Van Dun, Jacky Van Remoortere, Pieter Venet, Marc Wouters, Walter |
| description | The evaluation of structure–activity relationships associated with the modification of the R115777 quinolinone ring moiety displaying potent in vitro inhibiting activity is described.
The synthesis and inhibiting potency of farnesyltransferase inhibitors closely related to R115777 is reported. |
| doi_str_mv | 10.1016/S0960-894X(03)00180-X |
| format | article |
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The synthesis and inhibiting potency of farnesyltransferase inhibitors closely related to R115777 is reported.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/S0960-894X(03)00180-X</identifier><identifier>PMID: 12699751</identifier><language>eng</language><publisher>Oxford: Elsevier Ltd</publisher><subject>Alkyl and Aryl Transferases - antagonists & inhibitors ; Animals ; Antineoplastic agents ; Antineoplastic Agents - chemical synthesis ; Antineoplastic Agents - pharmacology ; Azepines - chemical synthesis ; Azepines - chemistry ; Azepines - pharmacology ; Biological and medical sciences ; Farnesyltranstransferase ; General aspects ; Humans ; In Vitro Techniques ; Indicators and Reagents ; Medical sciences ; Mice ; Microsomes, Liver - drug effects ; Microsomes, Liver - metabolism ; Pharmacology. Drug treatments ; Quinazolines - chemical synthesis ; Quinazolines - chemistry ; Quinazolines - pharmacology ; Quinolones - chemical synthesis ; Quinolones - chemistry ; Quinolones - pharmacology ; Structure-Activity Relationship ; Xenograft Model Antitumor Assays</subject><ispartof>Bioorganic & medicinal chemistry letters, 2003-05, Vol.13 (9), p.1543-1547</ispartof><rights>2003 Elsevier Science Ltd</rights><rights>2003 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c393t-15c3f6e51e52e8b6c6d72bcf15ba9c3594c3ab9d97e7e83fba3b5aa068d874c53</citedby><cites>FETCH-LOGICAL-c393t-15c3f6e51e52e8b6c6d72bcf15ba9c3594c3ab9d97e7e83fba3b5aa068d874c53</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27923,27924</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=14684598$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/12699751$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Angibaud, Patrick</creatorcontrib><creatorcontrib>Bourdrez, Xavier</creatorcontrib><creatorcontrib>Devine, Ann</creatorcontrib><creatorcontrib>End, David W</creatorcontrib><creatorcontrib>Freyne, Eddy</creatorcontrib><creatorcontrib>Ligny, Yannick</creatorcontrib><creatorcontrib>Muller, Philippe</creatorcontrib><creatorcontrib>Mannens, Geert</creatorcontrib><creatorcontrib>Pilatte, Isabelle</creatorcontrib><creatorcontrib>Poncelet, Virginie</creatorcontrib><creatorcontrib>Skrzat, Stacy</creatorcontrib><creatorcontrib>Smets, Gerda</creatorcontrib><creatorcontrib>Van Dun, Jacky</creatorcontrib><creatorcontrib>Van Remoortere, Pieter</creatorcontrib><creatorcontrib>Venet, Marc</creatorcontrib><creatorcontrib>Wouters, Walter</creatorcontrib><title>5-Imidazolyl-quinolinones, -quinazolinones and -benzo-azepinones as farnesyltransferase inhibitors</title><title>Bioorganic & medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>The evaluation of structure–activity relationships associated with the modification of the R115777 quinolinone ring moiety displaying potent in vitro inhibiting activity is described.
The synthesis and inhibiting potency of farnesyltransferase inhibitors closely related to R115777 is reported.</description><subject>Alkyl and Aryl Transferases - antagonists & inhibitors</subject><subject>Animals</subject><subject>Antineoplastic agents</subject><subject>Antineoplastic Agents - chemical synthesis</subject><subject>Antineoplastic Agents - pharmacology</subject><subject>Azepines - chemical synthesis</subject><subject>Azepines - chemistry</subject><subject>Azepines - pharmacology</subject><subject>Biological and medical sciences</subject><subject>Farnesyltranstransferase</subject><subject>General aspects</subject><subject>Humans</subject><subject>In Vitro Techniques</subject><subject>Indicators and Reagents</subject><subject>Medical sciences</subject><subject>Mice</subject><subject>Microsomes, Liver - drug effects</subject><subject>Microsomes, Liver - metabolism</subject><subject>Pharmacology. Drug treatments</subject><subject>Quinazolines - chemical synthesis</subject><subject>Quinazolines - chemistry</subject><subject>Quinazolines - pharmacology</subject><subject>Quinolones - chemical synthesis</subject><subject>Quinolones - chemistry</subject><subject>Quinolones - pharmacology</subject><subject>Structure-Activity Relationship</subject><subject>Xenograft Model Antitumor Assays</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2003</creationdate><recordtype>article</recordtype><recordid>eNqFkEtLxDAQgIMouj5-gtKLomA0aR5tTiLiCxY8qLC3kKRTjHTbNekKu7_e7EP36GHIZPJNZvgQOqbkihIqr1-JkgSXio_OCbsghJYEj7bQgHLJMeNEbKPBH7KH9mP8TBAnnO-iPZpLpQpBB8gK_Dz2lZl3zazBX1Pfdk2KFuJltrwuXlaFzLRVhi208w6bOUx-qzGrTUjZrOmDaWMNwUTIfPvhre-7EA_RTm2aCEfr8wC9P9y_3T3h4cvj893tEDumWI-pcKyWICiIHEornayK3LqaCmuUY0Jxx4xVlSqggJLV1jArjCGyrMqCO8EO0Nnq30novqYQez320UHTmBa6adQFy0lekCKBYgW60MUYoNaT4McmzDQleiFXL-XqhTlNmF7K1aPUd7IeMLVjqDZda5sJOF0DJjrT1EmH83HDcVlyocrE3aw4SDq-PQQdnYfWQeUDuF5Xnf9nlR8wBZnn</recordid><startdate>20030505</startdate><enddate>20030505</enddate><creator>Angibaud, Patrick</creator><creator>Bourdrez, Xavier</creator><creator>Devine, Ann</creator><creator>End, David W</creator><creator>Freyne, Eddy</creator><creator>Ligny, Yannick</creator><creator>Muller, Philippe</creator><creator>Mannens, Geert</creator><creator>Pilatte, Isabelle</creator><creator>Poncelet, Virginie</creator><creator>Skrzat, Stacy</creator><creator>Smets, Gerda</creator><creator>Van Dun, Jacky</creator><creator>Van Remoortere, Pieter</creator><creator>Venet, Marc</creator><creator>Wouters, Walter</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>7X8</scope></search><sort><creationdate>20030505</creationdate><title>5-Imidazolyl-quinolinones, -quinazolinones and -benzo-azepinones as farnesyltransferase inhibitors</title><author>Angibaud, Patrick ; Bourdrez, Xavier ; Devine, Ann ; End, David W ; Freyne, Eddy ; Ligny, Yannick ; Muller, Philippe ; Mannens, Geert ; Pilatte, Isabelle ; Poncelet, Virginie ; Skrzat, Stacy ; Smets, Gerda ; Van Dun, Jacky ; Van Remoortere, Pieter ; Venet, Marc ; Wouters, Walter</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c393t-15c3f6e51e52e8b6c6d72bcf15ba9c3594c3ab9d97e7e83fba3b5aa068d874c53</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2003</creationdate><topic>Alkyl and Aryl Transferases - antagonists & inhibitors</topic><topic>Animals</topic><topic>Antineoplastic agents</topic><topic>Antineoplastic Agents - chemical synthesis</topic><topic>Antineoplastic Agents - pharmacology</topic><topic>Azepines - chemical synthesis</topic><topic>Azepines - chemistry</topic><topic>Azepines - pharmacology</topic><topic>Biological and medical sciences</topic><topic>Farnesyltranstransferase</topic><topic>General aspects</topic><topic>Humans</topic><topic>In Vitro Techniques</topic><topic>Indicators and Reagents</topic><topic>Medical sciences</topic><topic>Mice</topic><topic>Microsomes, Liver - drug effects</topic><topic>Microsomes, Liver - metabolism</topic><topic>Pharmacology. Drug treatments</topic><topic>Quinazolines - chemical synthesis</topic><topic>Quinazolines - chemistry</topic><topic>Quinazolines - pharmacology</topic><topic>Quinolones - chemical synthesis</topic><topic>Quinolones - chemistry</topic><topic>Quinolones - pharmacology</topic><topic>Structure-Activity Relationship</topic><topic>Xenograft Model Antitumor Assays</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Angibaud, Patrick</creatorcontrib><creatorcontrib>Bourdrez, Xavier</creatorcontrib><creatorcontrib>Devine, Ann</creatorcontrib><creatorcontrib>End, David W</creatorcontrib><creatorcontrib>Freyne, Eddy</creatorcontrib><creatorcontrib>Ligny, Yannick</creatorcontrib><creatorcontrib>Muller, Philippe</creatorcontrib><creatorcontrib>Mannens, Geert</creatorcontrib><creatorcontrib>Pilatte, Isabelle</creatorcontrib><creatorcontrib>Poncelet, Virginie</creatorcontrib><creatorcontrib>Skrzat, Stacy</creatorcontrib><creatorcontrib>Smets, Gerda</creatorcontrib><creatorcontrib>Van Dun, Jacky</creatorcontrib><creatorcontrib>Van Remoortere, Pieter</creatorcontrib><creatorcontrib>Venet, Marc</creatorcontrib><creatorcontrib>Wouters, Walter</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>Bioorganic & medicinal chemistry letters</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Angibaud, Patrick</au><au>Bourdrez, Xavier</au><au>Devine, Ann</au><au>End, David W</au><au>Freyne, Eddy</au><au>Ligny, Yannick</au><au>Muller, Philippe</au><au>Mannens, Geert</au><au>Pilatte, Isabelle</au><au>Poncelet, Virginie</au><au>Skrzat, Stacy</au><au>Smets, Gerda</au><au>Van Dun, Jacky</au><au>Van Remoortere, Pieter</au><au>Venet, Marc</au><au>Wouters, Walter</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>5-Imidazolyl-quinolinones, -quinazolinones and -benzo-azepinones as farnesyltransferase inhibitors</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2003-05-05</date><risdate>2003</risdate><volume>13</volume><issue>9</issue><spage>1543</spage><epage>1547</epage><pages>1543-1547</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>The evaluation of structure–activity relationships associated with the modification of the R115777 quinolinone ring moiety displaying potent in vitro inhibiting activity is described.
The synthesis and inhibiting potency of farnesyltransferase inhibitors closely related to R115777 is reported.</abstract><cop>Oxford</cop><pub>Elsevier Ltd</pub><pmid>12699751</pmid><doi>10.1016/S0960-894X(03)00180-X</doi><tpages>5</tpages></addata></record> |
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| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 2003-05, Vol.13 (9), p.1543-1547 |
| issn | 0960-894X 1464-3405 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_73202707 |
| source | ScienceDirect Freedom Collection 2022-2024 |
| subjects | Alkyl and Aryl Transferases - antagonists & inhibitors Animals Antineoplastic agents Antineoplastic Agents - chemical synthesis Antineoplastic Agents - pharmacology Azepines - chemical synthesis Azepines - chemistry Azepines - pharmacology Biological and medical sciences Farnesyltranstransferase General aspects Humans In Vitro Techniques Indicators and Reagents Medical sciences Mice Microsomes, Liver - drug effects Microsomes, Liver - metabolism Pharmacology. Drug treatments Quinazolines - chemical synthesis Quinazolines - chemistry Quinazolines - pharmacology Quinolones - chemical synthesis Quinolones - chemistry Quinolones - pharmacology Structure-Activity Relationship Xenograft Model Antitumor Assays |
| title | 5-Imidazolyl-quinolinones, -quinazolinones and -benzo-azepinones as farnesyltransferase inhibitors |
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