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Synthesis of novel 1-aryl-3-[2,3- or 4-(thieno[3,2-b]pyridin-7-ylthio)phenyl]ureas and evaluation as VEGFR2 tyrosine kinase inhibitors

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dc.contributor.authorPeixoto, Daniela
dc.contributor.authorQueiroz, Maria João R.P.
dc.contributor.authorAbreu, Rui M.V.
dc.contributor.authorFroufe, Hugo J.C.
dc.contributor.authorCalhelha, Ricardo C.
dc.contributor.authorFerreira, Isabel C.F.R.
dc.date.accessioned2013-01-07T10:32:17Z
dc.date.available2013-01-07T10:32:17Z
dc.date.issued2012
dc.description.abstractVascular endothelial growth factor receptor 2 (VEGFR2) tyrosine kinase is involved in cancer and in angiogenesis. Herein, we report the synthesis of novel1-aryl-3-[2-, 3- or 4-{thieno[3,2-b ]pyridin-7-ylthio) phenyl]ureas as VEGFR2 inhibitors by promoting the regioselective attack of the thiol group of the 4-aminothiophenol in the chlorine nucleophilic displacement on 7-chlorothieno[3,2-b]pyridine 1, obtaining the aminated compounds Za- c. These were reacted with arylisocyanates to give the corresponding 1,3-diarylureas 3a-c, 4a-c and Sa-c (see scheme).
dc.identifier.citationPeixoto, Daniela; Queiroz, Maria João; Abreu, Rui M.V.; Froufe, Hugo; Calhelha, Ricardo C.; Ferreira, Isabel C.F.R. (2012). Synthesis of novel 1-aryl-3-[2,3- or 4-(thieno[3,2-b]pyridin-7-ylthio)phenyl]ureas and evaluation as VEGFR2 tyrosine kinase inhibitors. In XXIInd International Symposium on Medicinal Chemistry. Berlinpor
dc.identifier.urihttp://hdl.handle.net/10198/7835
dc.language.isoengpor
dc.peerreviewedyespor
dc.relationPEst-C/QUI/UI686/2011
dc.relationStrategic Project - UI 690 - 2011-2012
dc.titleSynthesis of novel 1-aryl-3-[2,3- or 4-(thieno[3,2-b]pyridin-7-ylthio)phenyl]ureas and evaluation as VEGFR2 tyrosine kinase inhibitorspor
dc.typeconference object
dspace.entity.typePublication
oaire.awardTitleStrategic Project - UI 690 - 2011-2012
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/PEst-OE%2FAGR%2FUI0690%2F2011/PT
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/SFRH/SFRH%2FBPD%2F68344%2F2010/PT
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/5876-PPCDTI/PTDC%2FQUI-QUI%2F111060%2F2009/PT
oaire.citation.conferencePlaceBerlim, Alemanhapor
oaire.citation.titleXXIInd International Symposium on Medicinal Chemistry, 2-6th September 2012por
oaire.fundingStream6817 - DCRRNI ID
oaire.fundingStreamSFRH
oaire.fundingStream5876-PPCDTI
person.familyNameAbreu
person.familyNameCalhelha
person.familyNameFerreira
person.givenNameRui M.V.
person.givenNameRicardo C.
person.givenNameIsabel C.F.R.
person.identifier144781
person.identifier.ciencia-id0F19-0DE2-12A2
person.identifier.ciencia-idF313-E3CE-554E
person.identifier.ciencia-id9418-CF95-9919
person.identifier.orcid0000-0002-7745-8015
person.identifier.orcid0000-0002-6801-4578
person.identifier.orcid0000-0003-4910-4882
person.identifier.ridJ-2172-2014
person.identifier.ridE-8500-2013
person.identifier.scopus-author-id7003290613
person.identifier.scopus-author-id6507978333
person.identifier.scopus-author-id36868826600
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.nameFundação para a Ciência e a Tecnologia
project.funder.nameFundação para a Ciência e a Tecnologia
project.funder.nameFundação para a Ciência e a Tecnologia
rcaap.rightsopenAccesspor
rcaap.typeconferenceObjectpor
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