Synthesis and kinase inhibitory potencies of new pyrido[3,4-g]quinazolines substituted at the 8-position

As part of the structure-activity relationship study undertaken around the pyrido[3,4-g]quinazoline moiety, new derivatives substituted at the 8-position were synthesized and evaluated regarding their ability to inhibit various protein kinases (CDK5, CLK1, DYRK1A, CK1, GSK3). Most active compound ex...

Full description

Saved in:
Bibliographic Details
Published in:ARKIVOC free online journal of organic chemistry 2020-07, Vol.2020 (7), p.105-116
Main Authors: Esvan, Yannick J., Josselin, Béatrice, Baratte, Blandine, Bach, Stéphane, Ruchaud, Sandrine, Anizon, Fabrice, Giraud, Francis, Moreau, Pascale
Format: Article
Language:English
Subjects:
Chemical Sciences
Citations: Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
cited_by cdi_FETCH-LOGICAL-c264t-5399489c3379293c4bee378668c194ea29c52f733dec168986863d18cd43111a3
cites
container_end_page 116
container_issue 7
container_start_page 105
container_title ARKIVOC free online journal of organic chemistry
container_volume 2020
creator Esvan, Yannick J.
Josselin, Béatrice
Baratte, Blandine
Bach, Stéphane
Ruchaud, Sandrine
Anizon, Fabrice
Giraud, Francis
Moreau, Pascale
description As part of the structure-activity relationship study undertaken around the pyrido[3,4-g]quinazoline moiety, new derivatives substituted at the 8-position were synthesized and evaluated regarding their ability to inhibit various protein kinases (CDK5, CLK1, DYRK1A, CK1, GSK3). Most active compound exhibited a nanomolar potency toward CLK1, demonstrating that substitution at 8-position is compatible with CLK1 inhibition.
doi_str_mv 10.24820/ark.5550190.p011.268
format article
fullrecord <record><control><sourceid>hal_cross</sourceid><recordid>TN_cdi_hal_primary_oai_HAL_hal_02926291v1</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>oai_HAL_hal_02926291v1</sourcerecordid><originalsourceid>FETCH-LOGICAL-c264t-5399489c3379293c4bee378668c194ea29c52f733dec168986863d18cd43111a3</originalsourceid><addsrcrecordid>eNpNkFFLwzAUhYMoOKc_QcirYGtu0qbJ4xjqhIEP6pNIyNLUxc2kNplSf72dG-LTPVy-cx4-hM6B5LQQlFzpbpWXZUlAkrwlADnl4gCNoCwhqwjQw3_5GJ3E-EbI0OTVCC0fep-WNrqIta_xynkdLXZ-6RYuha7HbUjWG2cjDg329gu3fefq8Mwui-z15WMzFL7D2vkBiJtFTC5tkq2xTniYxSJrQ3TJBX-Kjhq9jvZsf8fo6eb6cTrL5ve3d9PJPDOUFykrmZSFkIaxSlLJTLGwllWCc2FAFlZTaUraVIzV1gAXUnDBWQ3C1AUDAM3G6GK3u9Rr1XbuXXe9Ctqp2WSutj9CJeVUwicMbLljTRdi7GzzVwCiftWqQa3aq1VbtWpQy34Ahk9tsw</addsrcrecordid><sourcetype>Open Access Repository</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype></control><display><type>article</type><title>Synthesis and kinase inhibitory potencies of new pyrido[3,4-g]quinazolines substituted at the 8-position</title><source>Directory of Open Access Journals(OpenAccess)</source><creator>Esvan, Yannick J. ; Josselin, Béatrice ; Baratte, Blandine ; Bach, Stéphane ; Ruchaud, Sandrine ; Anizon, Fabrice ; Giraud, Francis ; Moreau, Pascale</creator><contributor>Muthyala, Ramaiah</contributor><creatorcontrib>Esvan, Yannick J. ; Josselin, Béatrice ; Baratte, Blandine ; Bach, Stéphane ; Ruchaud, Sandrine ; Anizon, Fabrice ; Giraud, Francis ; Moreau, Pascale ; Muthyala, Ramaiah</creatorcontrib><description>As part of the structure-activity relationship study undertaken around the pyrido[3,4-g]quinazoline moiety, new derivatives substituted at the 8-position were synthesized and evaluated regarding their ability to inhibit various protein kinases (CDK5, CLK1, DYRK1A, CK1, GSK3). Most active compound exhibited a nanomolar potency toward CLK1, demonstrating that substitution at 8-position is compatible with CLK1 inhibition.</description><identifier>ISSN: 1551-7012</identifier><identifier>ISSN: 1551-7004</identifier><identifier>EISSN: 1551-7012</identifier><identifier>DOI: 10.24820/ark.5550190.p011.268</identifier><language>eng</language><publisher>Arkat USA Inc</publisher><subject>Chemical Sciences</subject><ispartof>ARKIVOC free online journal of organic chemistry, 2020-07, Vol.2020 (7), p.105-116</ispartof><rights>Distributed under a Creative Commons Attribution 4.0 International License</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c264t-5399489c3379293c4bee378668c194ea29c52f733dec168986863d18cd43111a3</citedby><orcidid>0000-0002-2064-9558 ; 0000-0002-7186-7483 ; 0000-0001-7869-9622</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>230,314,780,784,864,885,27924,27925</link.rule.ids><backlink>$$Uhttps://hal.science/hal-02926291$$DView record in HAL$$Hfree_for_read</backlink></links><search><contributor>Muthyala, Ramaiah</contributor><creatorcontrib>Esvan, Yannick J.</creatorcontrib><creatorcontrib>Josselin, Béatrice</creatorcontrib><creatorcontrib>Baratte, Blandine</creatorcontrib><creatorcontrib>Bach, Stéphane</creatorcontrib><creatorcontrib>Ruchaud, Sandrine</creatorcontrib><creatorcontrib>Anizon, Fabrice</creatorcontrib><creatorcontrib>Giraud, Francis</creatorcontrib><creatorcontrib>Moreau, Pascale</creatorcontrib><title>Synthesis and kinase inhibitory potencies of new pyrido[3,4-g]quinazolines substituted at the 8-position</title><title>ARKIVOC free online journal of organic chemistry</title><description>As part of the structure-activity relationship study undertaken around the pyrido[3,4-g]quinazoline moiety, new derivatives substituted at the 8-position were synthesized and evaluated regarding their ability to inhibit various protein kinases (CDK5, CLK1, DYRK1A, CK1, GSK3). Most active compound exhibited a nanomolar potency toward CLK1, demonstrating that substitution at 8-position is compatible with CLK1 inhibition.</description><subject>Chemical Sciences</subject><issn>1551-7012</issn><issn>1551-7004</issn><issn>1551-7012</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2020</creationdate><recordtype>article</recordtype><recordid>eNpNkFFLwzAUhYMoOKc_QcirYGtu0qbJ4xjqhIEP6pNIyNLUxc2kNplSf72dG-LTPVy-cx4-hM6B5LQQlFzpbpWXZUlAkrwlADnl4gCNoCwhqwjQw3_5GJ3E-EbI0OTVCC0fep-WNrqIta_xynkdLXZ-6RYuha7HbUjWG2cjDg329gu3fefq8Mwui-z15WMzFL7D2vkBiJtFTC5tkq2xTniYxSJrQ3TJBX-Kjhq9jvZsf8fo6eb6cTrL5ve3d9PJPDOUFykrmZSFkIaxSlLJTLGwllWCc2FAFlZTaUraVIzV1gAXUnDBWQ3C1AUDAM3G6GK3u9Rr1XbuXXe9Ctqp2WSutj9CJeVUwicMbLljTRdi7GzzVwCiftWqQa3aq1VbtWpQy34Ahk9tsw</recordid><startdate>20200731</startdate><enddate>20200731</enddate><creator>Esvan, Yannick J.</creator><creator>Josselin, Béatrice</creator><creator>Baratte, Blandine</creator><creator>Bach, Stéphane</creator><creator>Ruchaud, Sandrine</creator><creator>Anizon, Fabrice</creator><creator>Giraud, Francis</creator><creator>Moreau, Pascale</creator><general>Arkat USA Inc</general><scope>AAYXX</scope><scope>CITATION</scope><scope>1XC</scope><orcidid>https://orcid.org/0000-0002-2064-9558</orcidid><orcidid>https://orcid.org/0000-0002-7186-7483</orcidid><orcidid>https://orcid.org/0000-0001-7869-9622</orcidid></search><sort><creationdate>20200731</creationdate><title>Synthesis and kinase inhibitory potencies of new pyrido[3,4-g]quinazolines substituted at the 8-position</title><author>Esvan, Yannick J. ; Josselin, Béatrice ; Baratte, Blandine ; Bach, Stéphane ; Ruchaud, Sandrine ; Anizon, Fabrice ; Giraud, Francis ; Moreau, Pascale</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c264t-5399489c3379293c4bee378668c194ea29c52f733dec168986863d18cd43111a3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2020</creationdate><topic>Chemical Sciences</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Esvan, Yannick J.</creatorcontrib><creatorcontrib>Josselin, Béatrice</creatorcontrib><creatorcontrib>Baratte, Blandine</creatorcontrib><creatorcontrib>Bach, Stéphane</creatorcontrib><creatorcontrib>Ruchaud, Sandrine</creatorcontrib><creatorcontrib>Anizon, Fabrice</creatorcontrib><creatorcontrib>Giraud, Francis</creatorcontrib><creatorcontrib>Moreau, Pascale</creatorcontrib><collection>CrossRef</collection><collection>Hyper Article en Ligne (HAL)</collection><jtitle>ARKIVOC free online journal of organic chemistry</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Esvan, Yannick J.</au><au>Josselin, Béatrice</au><au>Baratte, Blandine</au><au>Bach, Stéphane</au><au>Ruchaud, Sandrine</au><au>Anizon, Fabrice</au><au>Giraud, Francis</au><au>Moreau, Pascale</au><au>Muthyala, Ramaiah</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Synthesis and kinase inhibitory potencies of new pyrido[3,4-g]quinazolines substituted at the 8-position</atitle><jtitle>ARKIVOC free online journal of organic chemistry</jtitle><date>2020-07-31</date><risdate>2020</risdate><volume>2020</volume><issue>7</issue><spage>105</spage><epage>116</epage><pages>105-116</pages><issn>1551-7012</issn><issn>1551-7004</issn><eissn>1551-7012</eissn><abstract>As part of the structure-activity relationship study undertaken around the pyrido[3,4-g]quinazoline moiety, new derivatives substituted at the 8-position were synthesized and evaluated regarding their ability to inhibit various protein kinases (CDK5, CLK1, DYRK1A, CK1, GSK3). Most active compound exhibited a nanomolar potency toward CLK1, demonstrating that substitution at 8-position is compatible with CLK1 inhibition.</abstract><pub>Arkat USA Inc</pub><doi>10.24820/ark.5550190.p011.268</doi><tpages>12</tpages><orcidid>https://orcid.org/0000-0002-2064-9558</orcidid><orcidid>https://orcid.org/0000-0002-7186-7483</orcidid><orcidid>https://orcid.org/0000-0001-7869-9622</orcidid><oa>free_for_read</oa></addata></record>
fulltext fulltext
identifier ISSN: 1551-7012
ispartof ARKIVOC free online journal of organic chemistry, 2020-07, Vol.2020 (7), p.105-116
issn 1551-7012
1551-7004
1551-7012
language eng
recordid cdi_hal_primary_oai_HAL_hal_02926291v1
source Directory of Open Access Journals(OpenAccess)
subjects Chemical Sciences
title Synthesis and kinase inhibitory potencies of new pyrido[3,4-g]quinazolines substituted at the 8-position
url http://sfxeu10.hosted.exlibrisgroup.com/loughborough?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2025-01-01T03%3A07%3A33IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-hal_cross&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.genre=article&rft.atitle=Synthesis%20and%20kinase%20inhibitory%20potencies%20of%20new%20pyrido%5B3,4-g%5Dquinazolines%20substituted%20at%20the%208-position&rft.jtitle=ARKIVOC%20free%20online%20journal%20of%20organic%20chemistry&rft.au=Esvan,%20Yannick%20J.&rft.date=2020-07-31&rft.volume=2020&rft.issue=7&rft.spage=105&rft.epage=116&rft.pages=105-116&rft.issn=1551-7012&rft.eissn=1551-7012&rft_id=info:doi/10.24820/ark.5550190.p011.268&rft_dat=%3Chal_cross%3Eoai_HAL_hal_02926291v1%3C/hal_cross%3E%3Cgrp_id%3Ecdi_FETCH-LOGICAL-c264t-5399489c3379293c4bee378668c194ea29c52f733dec168986863d18cd43111a3%3C/grp_id%3E%3Coa%3E%3C/oa%3E%3Curl%3E%3C/url%3E&rft_id=info:oai/&rft_id=info:pmid/&rfr_iscdi=true