Publication
Synthesis of new N-[3-(thieno[3,2-b]pyridine-7-ylthio)phenyl]benzamides as potential inhibitors of VEGFR2 using rational design
| dc.contributor.author | Queiroz, Maria João R.P. | |
| dc.contributor.author | Begouin, Agathe | |
| dc.contributor.author | Campos, Joana F. | |
| dc.contributor.author | Peixoto, Daniela | |
| dc.contributor.author | Froufe, Hugo J.C. | |
| dc.contributor.author | Calhelha, Ricardo C. | |
| dc.contributor.author | Abreu, Rui M.V. | |
| dc.contributor.author | Ferreira, Isabel C.F.R. | |
| dc.date.accessioned | 2015-11-04T17:12:27Z | |
| dc.date.available | 2015-11-04T17:12:27Z | |
| dc.date.issued | 2013 | |
| dc.description.abstract | Vascular Endothelial Growth Factor Receptor 2 (VEGFR2) is the major receptor of the angiogenic effects when linked to VEGF released by tumors. It has a well known role as a transmembrane receptor activating multiple signaling pathways of proliferation and migration of endothelial cells [1], thus leading to the formation and the expansion of new blood vessels (vasculogenesis and angiogenesis) towards the tumor [2]. Therefore, several approaches have been developed to inhibit VEGFR activation and signaling [3]. Some thienopyridine derivatives have already been shown to be inhibitors of the tyrosine kinase domain of VEGFR2 preventing its activation [4]. Herein, we describe the synthesis of new N-[3-(thieno[3,2-b]pyridine-7 -ylthio )phenyl]benzamides, suggested by rational design as potential inhibitors of this domain, either through a Cu-catalyzed C-N coupling of a brominated di(hetero)arylthioether thieno[3,2-b]pyridine with benzamides, or through a reaction of an aminated di(hetero )arylthioether thieno[3,2-b ]pyridine with benzoyl chlorides, as presented below. The inhibition of the tyrosine kinase domain of VEGFR2 by the synthesized compounds will be evaluated by enzymatic and biomolecular assays using VEGF-stimulated Human Umbilical Vein Endothelial Cells (HUVECs). | pt_PT |
| dc.identifier.citation | Queiroz, Maria João R.P.; Begouin, Agathe; Campos, Joana F.; Peixoto, Daniela; Froufe, Hugo J.C.; Calhelha, Ricardo C.; Abreu, Rui M.V.; Ferreira, Isabel C.F.R. (2013). Synthesis of new N-[3-(thieno[3,2-b]pyridine-7-ylthio)phenyl]benzamides as potential inhibitors of VEGFR2 using rational design. In 49th International Conference on Medicinal Chemistry (RICT 2013). Nice | pt_PT |
| dc.identifier.uri | http://hdl.handle.net/10198/12278 | |
| dc.language.iso | eng | pt_PT |
| dc.peerreviewed | yes | pt_PT |
| dc.relation | PEst-C/QUI/UI686/2011 | pt_PT |
| dc.relation | Strategic Project - UI 690 - 2011-2012 | |
| dc.rights.uri | http://creativecommons.org/licenses/by/4.0/ | pt_PT |
| dc.title | Synthesis of new N-[3-(thieno[3,2-b]pyridine-7-ylthio)phenyl]benzamides as potential inhibitors of VEGFR2 using rational design | pt_PT |
| dc.type | conference object | |
| dspace.entity.type | Publication | |
| oaire.awardTitle | Strategic Project - UI 690 - 2011-2012 | |
| oaire.awardURI | info:eu-repo/grantAgreement/FCT/5876-PPCDTI/PTDC%2FQUI-QUI%2F111060%2F2009/PT | |
| oaire.awardURI | info:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/PEst-OE%2FAGR%2FUI0690%2F2011/PT | |
| oaire.awardURI | info:eu-repo/grantAgreement/FCT/SFRH/SFRH%2FBPD%2F36753%2F2007/PT | |
| oaire.awardURI | info:eu-repo/grantAgreement/FCT/SFRH/SFRH%2FBPD%2F68344%2F2010/PT | |
| oaire.citation.title | 49th International Conference on Medicinal Chemistry (RICT 2013) | pt_PT |
| oaire.fundingStream | 5876-PPCDTI | |
| oaire.fundingStream | 6817 - DCRRNI ID | |
| oaire.fundingStream | SFRH | |
| oaire.fundingStream | SFRH | |
| person.familyName | Calhelha | |
| person.familyName | Abreu | |
| person.familyName | Ferreira | |
| person.givenName | Ricardo C. | |
| person.givenName | Rui M.V. | |
| person.givenName | Isabel C.F.R. | |
| person.identifier | 144781 | |
| person.identifier.ciencia-id | F313-E3CE-554E | |
| person.identifier.ciencia-id | 0F19-0DE2-12A2 | |
| person.identifier.ciencia-id | 9418-CF95-9919 | |
| person.identifier.orcid | 0000-0002-6801-4578 | |
| person.identifier.orcid | 0000-0002-7745-8015 | |
| person.identifier.orcid | 0000-0003-4910-4882 | |
| person.identifier.rid | J-2172-2014 | |
| person.identifier.rid | E-8500-2013 | |
| person.identifier.scopus-author-id | 6507978333 | |
| person.identifier.scopus-author-id | 7003290613 | |
| person.identifier.scopus-author-id | 36868826600 | |
| project.funder.identifier | http://doi.org/10.13039/501100001871 | |
| project.funder.identifier | http://doi.org/10.13039/501100001871 | |
| project.funder.identifier | http://doi.org/10.13039/501100001871 | |
| project.funder.identifier | http://doi.org/10.13039/501100001871 | |
| project.funder.name | Fundação para a Ciência e a Tecnologia | |
| project.funder.name | Fundação para a Ciência e a Tecnologia | |
| project.funder.name | Fundação para a Ciência e a Tecnologia | |
| project.funder.name | Fundação para a Ciência e a Tecnologia | |
| rcaap.rights | openAccess | pt_PT |
| rcaap.type | conferenceObject | pt_PT |
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